S5749 |
Chlorpromazine
|
Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM. |
-
Nat Commun, 2024, 15(1):1669
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
|
|
S1333 |
Fluoxetine HCl
|
Fluoxetine HCl is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression. |
-
Int Immunopharmacol, 2024, 128:111524
-
Front Psychiatry, 2023, 14:1198502
-
Front Psychiatry, 2023, 14:1198502
|
|
S2493 |
Olanzapine
|
Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. |
-
Cell Commun Signal, 2024, 22(1):375
-
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
-
Pharmacol Res, 2021, 170:105714
|
|
S1975 |
Aripiprazole
|
Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist. |
-
Biomolecules, 2023, 10.3390/biom13091321
-
Biomolecules, 2023, 13(9)1321
-
J Lipid Res, 2022, 63(8):100249
|
|
S3024 |
Lamotrigine
|
Lamotrigine (BW-430C,LTG) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. |
-
Nat Commun, 2022, 13(1):2785
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S2346 |
Puerarin
|
Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist. |
-
Acta Biochim Biophys Sin (Shanghai), 2024, 56(2):270-279
-
Int J Mol Sci, 2023, 24(9)8328
-
Ecotoxicol Environ Saf, 2022, 247:114239
|
|
S2459 |
Clozapine
|
Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia. |
-
Alzheimers Dement, 2023, 10.1002/alz.13090
-
Redox Biol, 2023, 67:102915
-
Anticancer Res, 2021, 41(2):687-697
|
|
S2663 |
WAY-100635 Maleate
|
WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM. |
-
Med Sci Sports Exerc, 2022, 54(4):566-581
-
Sci Rep, 2021, 11(1):9300
-
J Pain, 2019, 20(1):16.e1-16.e16
|
|
S4244 |
Serotonin (5-HT) HCl
|
Serotonin (5-HT) HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist. |
-
Mod Pathol, 2022, 10.1038/s41379-022-01110-x
-
Med Sci Sports Exerc, 2022, 54(4):566-581
-
J Anim Sci, 2022, skac065
|
|
S2875 |
Prucalopride
|
Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes. |
-
Gut, 2019, 68(8):1406-1416
-
Front Pharmacol, 2019, 10:1491
-
Nutrients, 2017, 9(12)
|
|
S1444 |
Ziprasidone HCl
|
Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder. |
-
Anticancer Res, 2021, 41(2):687-697
-
Molecules, 2020, 25(18)E4206
-
Nature, 2018, 560(7718):372-376
|
|
S2677 |
BRL-15572 Dihydrochloride
|
BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. |
-
Brain Behav Immun, 2018, 74:49-67
-
Anesth Analg, 2018, 10.1213/ANE.0000000000003757
-
Int Immunopharmacol, 2018, 56:168-178
|
|
S4749 |
Citalopram HBr
|
Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM. |
-
Aging (Albany NY), 2021, 13(11):14729-14744
-
Viruses, 2021, 13(8)1533
-
Sci Rep, 2021, 11(1):1250
|
|
S2232 |
Ketanserin
|
Ketanserin (R41468, Ketanserinum) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug. |
-
Lab Invest, 2021, 1-14
-
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
-
Sci Rep, 2018, 8(1):15753
|
|
S2698 |
RS-127445
|
RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors. |
-
J Neuroinflammation, 2022, 19(1):23
-
Lab Invest, 2021, 1-14
-
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
|
|
S1243 |
Agomelatine (S20098)
|
Agomelatine (Valdoxan, Melitor, Thymanax,S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. |
-
Cells, 2022, 11(21)3467
-
Sci Rep, 2018, 8(1):15753
-
Neuropsychiatry (London), 2018, None
|
|
S1283 |
Asenapine maleate
|
Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder. |
-
J Adv Res, 2024, S2090-1232(24)00079-1
-
Cell Commun Signal, 2024, 22(1):266
-
Mol Cancer, 2023, 22(1):136
|
|
S2849 |
SB269970 HCl
|
SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. |
-
J Adv Res, 2024, S2090-1232(24)00079-1
-
Med Sci Sports Exerc, 2022, 54(4):566-581
-
Cancers (Basel), 2021, 13(21)5305
|
|
S2084 |
Duloxetine HCl
|
Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD). |
-
Cancers (Basel), 2022, 14(19)4883
-
Drug Metab Dispos, 2015, 44(3):378-88
-
J Pharmacol Exp Ther, 2014, 349(3):402-7
|
|
S4247 |
Prucalopride Succinate
|
Prucalopride(R-108512) is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively. |
-
Front Pharmacol, 2019, 10:1491
-
Front Pharmacol, 2018, 9:171
-
Neurogastroenterol Motil, 2018, 30(2)
|
|
S5857 |
Trazodone
|
Trazodone (AF-1161) is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders. |
-
Biomolecules, 2023, 10.3390/biom13091321
-
Biomolecules, 2023, 13(9)1321
-
J Lipid Res, 2022, 63(8):100249
|
|
S1615 |
Risperidone
|
Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder. |
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
-
Anticancer Res, 2021, 41(2):687-697
-
BMC Evol Biol, 2018, 18(1):89
|
|
S4053 |
Sertraline HCl
|
Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM. |
-
Antimicrob Agents Chemother, 2021, AAC.01146-20
-
Sci Rep, 2021, 11(1):1250
-
J Glob Antimicrob Resist, 2021, 27:167-171
|
|
S3183 |
Amitriptyline HCl
|
Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
-
PLoS Pathog, 2020, 16;16(3):e1008341
-
Sci Rep, 2018, 8(1):15753
|
|
S8183 |
Pimavanserin tartrate
|
Pimavanserin tartrate(ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease. |
-
Br J Pharmacol, 2021, 10.1111/bph.15756
-
Mol Ther Oncolytics, 2020, 19:19-32
-
ACS Chem Neurosci, 2020, 11(2):173-183
|
|
S0476 |
SCH-23390 hydrochloride
|
SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM. |
-
Theranostics, 2023, 13(10):3149-3164
-
JCI Insight, 2023, 8(16)e170434
-
JCI Insight, 2023, 8(16)e170434
|
|
S1483 |
Iloperidone
|
Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. |
-
Anticancer Res, 2021, 41(2):687-697
-
Sci Rep, 2018, 8(1):15753
|
|
S1345 |
Granisetron HCl
|
Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting. |
-
Redox Biol, 2023, 67:102889
-
Redox Biol, 2023, 67:102889
|
|
S2894 |
SB742457
|
SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2. |
-
Sci Rep, 2018, 8(1):15753
-
Sci Rep, 2017, 7(1):4983
|
|
S1390 |
Ondansetron HCl
|
Ondansetron HCl is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy. |
-
Immunity, 2019, 50(5):1163-1171
-
Int J Urol, 2016, 23(11):946-951
|
|
S3196 |
Azacyclonol
|
Azacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals. |
-
Bioengineered, 2021, 12(1):7446-7458
-
Oncol Rep, 2020, 44(6):2503-2516
|
|
S4249 |
Flopropione
|
Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist. |
-
SSRN, 2023, 17 Pages
-
Cells, 2022, 11(16)2585
-
Front Microbiol, 2020, 10:2936
|
|
S4259 |
Vilazodone HCl
|
Vilazodone HCl(EMD68843,SB659746A) is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder. |
-
J Pain, 2019, 20(1):16.e1-16.e16
-
Acta Pol Pharm, 2017, 74(3):765-775
|
|
S2096 |
Almotriptan Malate
|
Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. |
-
Oncotarget, 2017, 9(3):3507-3518
-
Oncotarget, 2016, 7(9):9975-92
|
|
S5401 |
Tegaserod Maleate
|
Tegaserod Maleate(HTF-919) is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors. |
-
Cancers (Basel), 2022, 14(15)3592
-
Front Oncol, 2021, 11:683241
|
|
S3821 |
Nuciferine
|
Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor. |
-
Antioxidants (Basel), 2024, 13(6)714
-
Br J Pharmacol, 2021, 178(5):1182-1199
-
Tohoku J Exp Med, 2021, 254(1):17-23
|
|
S5949 |
Metoclopramide hydrochloride hydrate
|
Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic. |
-
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
-
Pharmazie, 2021, 76(4):172-174
|
|
S5714 |
lurasidone
|
Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors. |
-
Alzheimers Dement, 2023, 10.1002/alz.13090
-
Chem Biol Drug Des, 2022, 100(5):699-721
|
|
S4358 |
Pimozide
|
Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity. |
-
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
-
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
|
|
S4377 |
Imipramine HCl
|
Imipramine (Melipramine,G 22355) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination). |
-
Cancer Drug Resist, 2022, 5(3):612-624
-
Antioxidants (Basel), 2021, 10(6)956
|
|
S1432 |
Sumatriptan Succinate
|
Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches. |
-
J Toxicol Sci, 2017, 42(6):755-761
|
|
S2112 |
Blonanserin
|
Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia. |
-
Sci Rep, 2018, 8(1):15753
|
|
S1649 |
Zolmitriptan
|
Zolmitriptan(BW-311C90) is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines. |
-
Int J Pharm, 2019, 560:294-305
|
|
S8010 |
PRX-08066 Maleic acid
|
PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2. |
-
Clin Exp Metastasis, 2018, 35(3):123-134
|
|
S4064 |
Escitalopram Oxalate
|
Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM. |
-
J Matern Fetal Neonatal Med, 2023, 36(1):2183468
|
|
S4086 |
Loxapine Succinate
|
Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. |
-
Anticancer Res, 2021, 41(2):687-697
|
|
S1996 |
Ondansetron
|
Ondansetron (GR 38032F, GR-C507/75,SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic. |
-
Int J Urol, 2016, 23(11):946-951
|
|
S2856 |
SB 271046 hydrochloride
|
SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes. |
-
Sci Rep, 2018, 8(1):15753
|
|
S0723 |
BRL 15572
|
BRL-15572 is a preferential antagonist at native human 5-HT1D receptors, can be a useful tool for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies. |
-
J Neuroinflammation, 2022, 19(1):205
|
|
S2852 |
BRL-54443
|
BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. |
-
bioRxiv, 2024, 10.1101/2024.01.28.577572
-
Theranostics, 2021, 11(14):6950-6965
|
|
S4889 |
Perospirone hydrochloride
|
Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist. |
-
J Med Virol, 2023, 95(6):e28856
-
J Med Virol, 2023, 95(6):e28856
|
|
S3817 |
Harmine hydrochloride
|
Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM. |
-
Cancers (Basel), 2022, 14(2)326
|
|
S3054 |
Alverine Citrate
|
Alverine citrate (NSC 35459) is a drug used for functional gastrointestinal disorders. Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM. |
-
Am J Physiol Lung Cell Mol Physiol, 2018, 315(2):L133-L148
|
|
S5947 |
Amitriptyline
|
Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid. |
-
Cancers (Basel), 2019, 11(12)
|
|
S4635 |
Cyproheptadine hydrochloride sesquihydrate
|
Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor. |
-
Anticancer Res, 2019, 39(7):3767-3775
|
|
S4256 |
Buspirone HCl
|
Buspirone(Buspirone hydrochloride) is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. |
-
Food Chem Toxicol, 2020, 30;141:111394
|
|
S4751 |
Cisapride hydrate
|
Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic. |
-
Elife, 2021, 10e68714
|
|
S4694 |
Alosetron Hydrochloride
|
Alosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. |
-
Eur J Pharmacol, 2024, 979:176835
-
Cell, 2017, 170(1):185-198
|
|
S3716 |
Flibanserin
|
Flibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors. |
-
Arch Biochem Biophys, 2024, 754:109958
-
Nat Commun, 2021, 12(1):5919
|
|
S3723 |
Ramosetron Hydrochloride
|
Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. |
-
Theranostics, 2020, 10(16):7351-7368
|
|
S2582 |
Trazodone HCl
|
Trazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders. |
-
J Lipid Res, 2022, 63(8):100249
|
|
S5563 |
Thioridazine hydrochloride
|
Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent. |
-
Cell Syst, 2019, 8(2):97-108
|
|
S5858 |
Vilazodone
|
Vilazodone (EMD-68843, SB-659746A) is a novel antidepressant having a selective serotonin (5-HT) reuptake inhibitory and 5-HT1A receptor partial agonist activity. The affinity of vilazodone is much higher in the 5-HT reuptake site (Ki=0.1 nM) than in norepinephrine (Ki=56 nM) and dopamine (Ki=37 nM) sites. |
-
J Pain, 2019, 20(1):16.e1-16.e16
|
|
S1245 |
Latrepirdine 2HCl
|
Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
|
|
S1869 |
Dapoxetine HCl
|
Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation. |
|
|
S1488 |
Naratriptan HCl
|
Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches. |
|
|
S2691 |
BMY 7378 Dihydrochloride
|
BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3. |
|
|
S1607 |
Rizatriptan Benzoate
|
Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks. |
|
|
S1385 |
Mosapride Citrate
|
Mosapride Citrate (TAK-370, AS-4370, Gasmotin) is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
|
|
S2016 |
Mirtazapine
|
Mirtazapine (Org3770,6-Azamianserin) is an adrenergic and seroton receptor antagonist, used to treat depression. |
|
|
S1898 |
Tropisetron HCl
|
Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy. |
|
|
S3180 |
Eletriptan HBr
|
Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively. |
|
|
S1394 |
Pizotifen Malate
|
Pizotifen Malate (Sandomigran, pizotyline,BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches. |
|
|
S2106 |
Azasetron HCl
|
Azasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. |
|
|
S5741 |
Quetiapine
|
Quetiapine(ICI204636) is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55. |
|
|
S0496 |
PF-04995274
|
PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. |
|
|
S5848 |
Frovatriptan Succinate
|
Frovatriptan Succinate(SB 209509 Succinate,VML 251 Succinate) is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors. |
|
|
S5326 |
Dolasetron
|
Dolasetron(MDL-73147EF) is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors. |
|
|
S5472 |
Nafronyl oxalate salt
|
Nafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders. |
|
|
S5153 |
Tetrahydroberberine
|
Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors. |
|
|
S5253 |
Cisapride (R 51619)
|
Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects. |
|
|
S0939 |
γ-Mangostin
|
γ-Mangostin (Gamma-Mangostin) is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, which can reduce the perfusion pressure response of rat coronary artery to 5-HT2A with an IC50 of 0.32 µM and inhibit [3H] spiperone binding to cultured rat aortic myocytes with an IC50 of 3.5 nM. Gamma-Mangostin is also an inhibitor of Transthyretin (TTR) fibrillization. |
|
|
S3050 |
Palonosetron HCl
|
Palonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. |
|
|
S0282 |
YL 0919
|
YL0919, a novel structure compound, exerts dual effect on the serotonergic system, as both 5-hydroxytryptamine receptor 1A (5-HT1A) agonist and 5-HT uptake blocker, showing remarkable antidepressant effects in animal models. |
|
|
S9239 |
Isocorynoxeine
|
Isocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. Isocorynoxeine suppress 5-HT2A receptor-mediated current response with IC50 of 72.4 μM. |
|
|
S6324 |
5-Methoxytryptamine
|
5-Methoxytryptamine (Mexamine, Methoxytryptamine) is a tryptamine derivative that acts as a full agonist at the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors. |
|
|
S2865 |
VUF 10166
|
VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower. |
|
|
E4835New |
Sumatriptan
|
Sumatriptan (GR43175) is a selective agonist of 5-HT1D receptor, which is effectively used in the acute treatment of migraine. It causes a vasopressor response in the systemic and pulmonary arterial circulations and coronary artery vasoconstriction. |
|
|
S7538 |
RS-102895 Hydrochloride
|
RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively. |
|
|
S0313 |
Volinanserin
|
Volinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity. |
|
|
S9258 |
(+)-Isocorynoline
|
Isocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. |
|
|
S0318 |
Ansofaxine hydrochloride
|
Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively. |
|
|
E4477New |
Lumateperone
|
Lumateperone (ITI-007) is an antagonist of 5-HT2A receptor with Ki of 0.54 nM. It has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia. |
|
|
S3510 |
NLX-101
|
NLX-101 (F-15599) is a highly selective 5-HT1A receptor biased agonist that mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors. |
|
|
S5185 |
Perospirone
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively. |
|
|
S0779 |
Pirenperone
|
Pirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg). |
|
|
E4856New |
Rotigotine Hydrochloride
|
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a potent Agonist of dopamine receptor, with Ki values of 0.71 nM for dopamine D3 receptor, 4-15 nM for D2, D5, D4 receptors, and 83 nM for dopamine D1 receptor. It also acts as a partial agonist of the 5-HT1A receptor, and as an antagonist of the α2B-adrenergic receptor. |
|
|
S5398 |
Nefazodone hydrochloride
|
Nefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake. |
|
|
E4851New |
Tandospirone citrate
|
Tandospirone citrate, is a potent, selective and a partial agonist of the 5-HT1A receptor. It exhibited good permeability in the intestine, with passive diffusion being the main mode of drug absorption, it also has anxiolytic effects and can be used in generalized anxiety disorder treatments. |
|
|
S4740 |
Sodium ferulate
|
Sodium ferulate (SF, Ferulic acid sodium salt), the sodium salt of ferulic acid, is a drug used in traditional Chinese medicine for treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis. |
|
|
E4840New |
Ziprasidone hydrochloride monohydrate
|
Ziprasidone hydrochloride monohydrate is an antipsychotic drug, a combined antagonist of 5-HT (serotonin) and dopamine receptor. It exhibits binding affinities for D2, 5-HT2A, 5-HT1A with Ki values 4.8 nM, 0.42 nM, 3.4 nM respectively. |
|
|
S8447 |
8-OH-DPAT (8-Hydroxy-DPAT)
|
8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous. |
|
|
S5965 |
Urapidil
|
Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist. |
|
|
E0070 |
4F 4PP oxalate
|
4F 4PP oxalate is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 5.3 nM), which is selective for 5-HT2A receptors over 5-HT1C receptors (Ki = 620 nM). |
|
|
S2649 |
SB 200646
|
SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo. |
|
|
S1642 |
Methyldopa
|
Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. |
|
|
E4812New |
Fluoxetine
|
Fluoxetine (LY-110140 free base) is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine is used widely in the treatment of depression, anxiety-related symptoms and also displays anticonvulsant activity. |
|
|
E4870New |
Naratriptan
|
Naratriptan is an agonist of 5-hydroxytryptamine1B/D (5-HT1B/D) receptors, which reduces the frequency of cluster headache. |
|
|
E4866New |
Paroxetine
|
Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) used to treat depression and anxiety disorders. It inhibits pyroptosis and reduces osteoclast formation by blocking the NF-κB signalling pathway. |
|
|
S0104 |
Pardoprunox (SLV-308) hydrochloride
|
Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively. |
|
|
S3913 |
Pimethixene maleate
|
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. |
|
|
S5770 |
Pizotifen
|
Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site. |
|
|
S0113 |
Eptapirone
|
Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.The affinity (pKi) of F11440 for 5-HT1A binding sites is 8.33.
|
|
|
S4839 |
Mosapride
|
Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
|
|
S9039 |
Albiflorin
|
Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity. |
|
|
S4748 |
Ondansetron Hydrochloride Dihydrate
|
Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors. |
|
|
S3706 |
Sarpogrelate hydrochloride
|
Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively. |
|
|
S6087 |
Indophagolin
|
Indophagolin, a potent indoline-containing autophagy inhibitor with IC50 of 140 nM, antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively, also has a strong antagonistic effect on serotonin receptor 5-HT6 with IC50 of 1.0 μM. |
|
|
S5485 |
Desipramine Hydrochloride
|
Desipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects. |
|
|
S5538 |
Tropisetron
|
Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
-
Chin Med, 2024, 19(1):87
-
Neural Regen Res, 2023, 18(9):2019-2028
|
|
S2025 |
Urapidil HCl
|
Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. |
|
|
E2356 |
Tandospirone
|
Tandospirone (SM-3997), a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM, has anxiolytic and antidepressant activities. |
|
|
S6465 |
Tafamidis
|
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. |
|
|
S5071 |
Duloxetine
|
Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake. |
|
|
S5843 |
Cinitapride Hydrogen Tartrate
|
Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors |
|
|
S0893 |
SB-200646A
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. |
|
|
S2644 |
Lerisetron
|
Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM. |
|
|
S2578 |
1-Phenylbiguanide
|
1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM. |
|
|
S5428 |
Promazine hydrochloride
|
Promazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects. |
|
|
S0222 |
Lvguidingan
|
Lvguidingan (Anticonvulsant 7903, 3,4-dichlorophenyl propenylisobutylamide) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain. |
|
|
S4283 |
Cyclobenzaprine HCl
|
Cyclobenzaprine HCl(Cyclobenzaprine hydrochloride) is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.
|
|
|
S5052 |
Granisetron
|
Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy. |
-
Neural Regen Res, 2023, 18(9):2047-2055
|
|
S9510 |
Protriptyline hydrochloride
|
Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake. |
|
|
S2669 |
LY310762 HCl
|
LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor. |
|
|
S3175 |
Atomoxetine HCl
|
Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters. |
|
|
S9174 |
Xanthotoxol
|
Xanthotoxol (8-Hydroxypsoralen, 8-Hydroxypsoralene, 8-Hydroxyfuranocoumarin, Psoralen), a biologically active linear furocoumarin found in a large number of plants, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects. |
|
|
S5740 |
Palonosetron
|
Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). |
|
|
S5060 |
Metadoxine
|
Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD. |
|
|
S1333 |
Fluoxetine HCl
|
Fluoxetine HCl is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression. |
- Int Immunopharmacol, 2024, 128:111524
- Front Psychiatry, 2023, 14:1198502
- Front Psychiatry, 2023, 14:1198502
|
|
S3024 |
Lamotrigine
|
Lamotrigine (BW-430C,LTG) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. |
- Nat Commun, 2022, 13(1):2785
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S4749 |
Citalopram HBr
|
Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM. |
- Aging (Albany NY), 2021, 13(11):14729-14744
- Viruses, 2021, 13(8)1533
- Sci Rep, 2021, 11(1):1250
|
|
S2084 |
Duloxetine HCl
|
Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD). |
- Cancers (Basel), 2022, 14(19)4883
- Drug Metab Dispos, 2015, 44(3):378-88
- J Pharmacol Exp Ther, 2014, 349(3):402-7
|
|
S4053 |
Sertraline HCl
|
Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM. |
- Antimicrob Agents Chemother, 2021, AAC.01146-20
- Sci Rep, 2021, 11(1):1250
- J Glob Antimicrob Resist, 2021, 27:167-171
|
|
S3183 |
Amitriptyline HCl
|
Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
- Environ Toxicol Chem, 2021, 10.1002/etc.5018
- PLoS Pathog, 2020, 16;16(3):e1008341
- Sci Rep, 2018, 8(1):15753
|
|
S8183 |
Pimavanserin tartrate
|
Pimavanserin tartrate(ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease. |
- Br J Pharmacol, 2021, 10.1111/bph.15756
- Mol Ther Oncolytics, 2020, 19:19-32
- ACS Chem Neurosci, 2020, 11(2):173-183
|
|
S1483 |
Iloperidone
|
Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. |
- Anticancer Res, 2021, 41(2):687-697
- Sci Rep, 2018, 8(1):15753
|
|
S4377 |
Imipramine HCl
|
Imipramine (Melipramine,G 22355) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination). |
- Cancer Drug Resist, 2022, 5(3):612-624
- Antioxidants (Basel), 2021, 10(6)956
|
|
S4064 |
Escitalopram Oxalate
|
Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM. |
- J Matern Fetal Neonatal Med, 2023, 36(1):2183468
|
|
S3817 |
Harmine hydrochloride
|
Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM. |
- Cancers (Basel), 2022, 14(2)326
|
|
S2582 |
Trazodone HCl
|
Trazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders. |
- J Lipid Res, 2022, 63(8):100249
|
|
S5563 |
Thioridazine hydrochloride
|
Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent. |
- Cell Syst, 2019, 8(2):97-108
|
|
S1869 |
Dapoxetine HCl
|
Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation. |
|
|
S0282 |
YL 0919
|
YL0919, a novel structure compound, exerts dual effect on the serotonergic system, as both 5-hydroxytryptamine receptor 1A (5-HT1A) agonist and 5-HT uptake blocker, showing remarkable antidepressant effects in animal models. |
|
|
S9239 |
Isocorynoxeine
|
Isocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. Isocorynoxeine suppress 5-HT2A receptor-mediated current response with IC50 of 72.4 μM. |
|
|
S9258 |
(+)-Isocorynoline
|
Isocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. |
|
|
S0318 |
Ansofaxine hydrochloride
|
Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively. |
|
|
S1642 |
Methyldopa
|
Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. |
|
|
E4812New |
Fluoxetine
|
Fluoxetine (LY-110140 free base) is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine is used widely in the treatment of depression, anxiety-related symptoms and also displays anticonvulsant activity. |
|
|
E4866New |
Paroxetine
|
Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) used to treat depression and anxiety disorders. It inhibits pyroptosis and reduces osteoclast formation by blocking the NF-κB signalling pathway. |
|
|
S3913 |
Pimethixene maleate
|
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. |
|
|
S9039 |
Albiflorin
|
Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity. |
|
|
S5485 |
Desipramine Hydrochloride
|
Desipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects. |
|
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S6465 |
Tafamidis
|
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. |
|
|
S5071 |
Duloxetine
|
Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake. |
|
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S9510 |
Protriptyline hydrochloride
|
Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake. |
|
|
S3175 |
Atomoxetine HCl
|
Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters. |
|
|
S5749 |
Chlorpromazine
|
Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM. |
- Nat Commun, 2024, 15(1):1669
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
|
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S2493 |
Olanzapine
|
Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. |
- Cell Commun Signal, 2024, 22(1):375
- Nat Protoc, 2021, 10.1038/s41596-021-00624-z
- Pharmacol Res, 2021, 170:105714
|
|
S2346 |
Puerarin
|
Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist. |
- Acta Biochim Biophys Sin (Shanghai), 2024, 56(2):270-279
- Int J Mol Sci, 2023, 24(9)8328
- Ecotoxicol Environ Saf, 2022, 247:114239
|
|
S2459 |
Clozapine
|
Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia. |
- Alzheimers Dement, 2023, 10.1002/alz.13090
- Redox Biol, 2023, 67:102915
- Anticancer Res, 2021, 41(2):687-697
|
|
S2663 |
WAY-100635 Maleate
|
WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM. |
- Med Sci Sports Exerc, 2022, 54(4):566-581
- Sci Rep, 2021, 11(1):9300
- J Pain, 2019, 20(1):16.e1-16.e16
|
|
S1444 |
Ziprasidone HCl
|
Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder. |
- Anticancer Res, 2021, 41(2):687-697
- Molecules, 2020, 25(18)E4206
- Nature, 2018, 560(7718):372-376
|
|
S2677 |
BRL-15572 Dihydrochloride
|
BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. |
- Brain Behav Immun, 2018, 74:49-67
- Anesth Analg, 2018, 10.1213/ANE.0000000000003757
- Int Immunopharmacol, 2018, 56:168-178
|
|
S2232 |
Ketanserin
|
Ketanserin (R41468, Ketanserinum) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug. |
- Lab Invest, 2021, 1-14
- Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
- Sci Rep, 2018, 8(1):15753
|
|
S2698 |
RS-127445
|
RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors. |
- J Neuroinflammation, 2022, 19(1):23
- Lab Invest, 2021, 1-14
- Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
|
|
S1243 |
Agomelatine (S20098)
|
Agomelatine (Valdoxan, Melitor, Thymanax,S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. |
- Cells, 2022, 11(21)3467
- Sci Rep, 2018, 8(1):15753
- Neuropsychiatry (London), 2018, None
|
|
S1283 |
Asenapine maleate
|
Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder. |
- J Adv Res, 2024, S2090-1232(24)00079-1
- Cell Commun Signal, 2024, 22(1):266
- Mol Cancer, 2023, 22(1):136
|
|
S2849 |
SB269970 HCl
|
SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. |
- J Adv Res, 2024, S2090-1232(24)00079-1
- Med Sci Sports Exerc, 2022, 54(4):566-581
- Cancers (Basel), 2021, 13(21)5305
|
|
S5857 |
Trazodone
|
Trazodone (AF-1161) is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders. |
- Biomolecules, 2023, 10.3390/biom13091321
- Biomolecules, 2023, 13(9)1321
- J Lipid Res, 2022, 63(8):100249
|
|
S1615 |
Risperidone
|
Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder. |
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
- Anticancer Res, 2021, 41(2):687-697
- BMC Evol Biol, 2018, 18(1):89
|
|
S1345 |
Granisetron HCl
|
Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting. |
- Redox Biol, 2023, 67:102889
- Redox Biol, 2023, 67:102889
|
|
S2894 |
SB742457
|
SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2. |
- Sci Rep, 2018, 8(1):15753
- Sci Rep, 2017, 7(1):4983
|
|
S1390 |
Ondansetron HCl
|
Ondansetron HCl is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy. |
- Immunity, 2019, 50(5):1163-1171
- Int J Urol, 2016, 23(11):946-951
|
|
S4249 |
Flopropione
|
Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist. |
- SSRN, 2023, 17 Pages
- Cells, 2022, 11(16)2585
- Front Microbiol, 2020, 10:2936
|
|
S3821 |
Nuciferine
|
Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor. |
- Antioxidants (Basel), 2024, 13(6)714
- Br J Pharmacol, 2021, 178(5):1182-1199
- Tohoku J Exp Med, 2021, 254(1):17-23
|
|
S5714 |
lurasidone
|
Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors. |
- Alzheimers Dement, 2023, 10.1002/alz.13090
- Chem Biol Drug Des, 2022, 100(5):699-721
|
|
S4358 |
Pimozide
|
Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity. |
- Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
- Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
|
|
S2112 |
Blonanserin
|
Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia. |
- Sci Rep, 2018, 8(1):15753
|
|
S8010 |
PRX-08066 Maleic acid
|
PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2. |
- Clin Exp Metastasis, 2018, 35(3):123-134
|
|
S4086 |
Loxapine Succinate
|
Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. |
- Anticancer Res, 2021, 41(2):687-697
|
|
S1996 |
Ondansetron
|
Ondansetron (GR 38032F, GR-C507/75,SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic. |
- Int J Urol, 2016, 23(11):946-951
|
|
S2856 |
SB 271046 hydrochloride
|
SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes. |
- Sci Rep, 2018, 8(1):15753
|
|
S0723 |
BRL 15572
|
BRL-15572 is a preferential antagonist at native human 5-HT1D receptors, can be a useful tool for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies. |
- J Neuroinflammation, 2022, 19(1):205
|
|
S4889 |
Perospirone hydrochloride
|
Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist. |
- J Med Virol, 2023, 95(6):e28856
- J Med Virol, 2023, 95(6):e28856
|
|
S3054 |
Alverine Citrate
|
Alverine citrate (NSC 35459) is a drug used for functional gastrointestinal disorders. Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM. |
- Am J Physiol Lung Cell Mol Physiol, 2018, 315(2):L133-L148
|
|
S5947 |
Amitriptyline
|
Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid. |
- Cancers (Basel), 2019, 11(12)
|
|
S4635 |
Cyproheptadine hydrochloride sesquihydrate
|
Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor. |
- Anticancer Res, 2019, 39(7):3767-3775
|
|
S4694 |
Alosetron Hydrochloride
|
Alosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. |
- Eur J Pharmacol, 2024, 979:176835
- Cell, 2017, 170(1):185-198
|
|
S3723 |
Ramosetron Hydrochloride
|
Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. |
- Theranostics, 2020, 10(16):7351-7368
|
|
S1245 |
Latrepirdine 2HCl
|
Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
|
|
S2016 |
Mirtazapine
|
Mirtazapine (Org3770,6-Azamianserin) is an adrenergic and seroton receptor antagonist, used to treat depression. |
|
|
S1898 |
Tropisetron HCl
|
Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy. |
|
|
S1394 |
Pizotifen Malate
|
Pizotifen Malate (Sandomigran, pizotyline,BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches. |
|
|
S2106 |
Azasetron HCl
|
Azasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. |
|
|
S5326 |
Dolasetron
|
Dolasetron(MDL-73147EF) is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors. |
|
|
S5472 |
Nafronyl oxalate salt
|
Nafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders. |
|
|
S0939 |
γ-Mangostin
|
γ-Mangostin (Gamma-Mangostin) is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, which can reduce the perfusion pressure response of rat coronary artery to 5-HT2A with an IC50 of 0.32 µM and inhibit [3H] spiperone binding to cultured rat aortic myocytes with an IC50 of 3.5 nM. Gamma-Mangostin is also an inhibitor of Transthyretin (TTR) fibrillization. |
|
|
S3050 |
Palonosetron HCl
|
Palonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. |
|
|
S2865 |
VUF 10166
|
VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower. |
|
|
S7538 |
RS-102895 Hydrochloride
|
RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively. |
|
|
S0313 |
Volinanserin
|
Volinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity. |
|
|
E4477New |
Lumateperone
|
Lumateperone (ITI-007) is an antagonist of 5-HT2A receptor with Ki of 0.54 nM. It has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia. |
|
|
S5185 |
Perospirone
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively. |
|
|
S0779 |
Pirenperone
|
Pirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg). |
|
|
S5398 |
Nefazodone hydrochloride
|
Nefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake. |
|
|
E4840New |
Ziprasidone hydrochloride monohydrate
|
Ziprasidone hydrochloride monohydrate is an antipsychotic drug, a combined antagonist of 5-HT (serotonin) and dopamine receptor. It exhibits binding affinities for D2, 5-HT2A, 5-HT1A with Ki values 4.8 nM, 0.42 nM, 3.4 nM respectively. |
|
|
E0070 |
4F 4PP oxalate
|
4F 4PP oxalate is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 5.3 nM), which is selective for 5-HT2A receptors over 5-HT1C receptors (Ki = 620 nM). |
|
|
S2649 |
SB 200646
|
SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo. |
|
|
S5770 |
Pizotifen
|
Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site. |
|
|
S4748 |
Ondansetron Hydrochloride Dihydrate
|
Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors. |
|
|
S3706 |
Sarpogrelate hydrochloride
|
Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively. |
|
|
S6087 |
Indophagolin
|
Indophagolin, a potent indoline-containing autophagy inhibitor with IC50 of 140 nM, antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively, also has a strong antagonistic effect on serotonin receptor 5-HT6 with IC50 of 1.0 μM. |
|
|
S5538 |
Tropisetron
|
Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
- Chin Med, 2024, 19(1):87
- Neural Regen Res, 2023, 18(9):2019-2028
|
|
S0893 |
SB-200646A
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. |
|
|
S2644 |
Lerisetron
|
Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM. |
|
|
S5428 |
Promazine hydrochloride
|
Promazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects. |
|
|
S4283 |
Cyclobenzaprine HCl
|
Cyclobenzaprine HCl(Cyclobenzaprine hydrochloride) is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.
|
|
|
S5052 |
Granisetron
|
Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy. |
- Neural Regen Res, 2023, 18(9):2047-2055
|
|
S2669 |
LY310762 HCl
|
LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor. |
|
|
S9174 |
Xanthotoxol
|
Xanthotoxol (8-Hydroxypsoralen, 8-Hydroxypsoralene, 8-Hydroxyfuranocoumarin, Psoralen), a biologically active linear furocoumarin found in a large number of plants, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects. |
|
|
S5740 |
Palonosetron
|
Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). |
|
|
S5060 |
Metadoxine
|
Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD. |
|
|
S1975 |
Aripiprazole
|
Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist. |
- Biomolecules, 2023, 10.3390/biom13091321
- Biomolecules, 2023, 13(9)1321
- J Lipid Res, 2022, 63(8):100249
|
|
S4244 |
Serotonin (5-HT) HCl
|
Serotonin (5-HT) HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist. |
- Mod Pathol, 2022, 10.1038/s41379-022-01110-x
- Med Sci Sports Exerc, 2022, 54(4):566-581
- J Anim Sci, 2022, skac065
|
|
S2875 |
Prucalopride
|
Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes. |
- Gut, 2019, 68(8):1406-1416
- Front Pharmacol, 2019, 10:1491
- Nutrients, 2017, 9(12)
|
|
S4247 |
Prucalopride Succinate
|
Prucalopride(R-108512) is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively. |
- Front Pharmacol, 2019, 10:1491
- Front Pharmacol, 2018, 9:171
- Neurogastroenterol Motil, 2018, 30(2)
|
|
S0476 |
SCH-23390 hydrochloride
|
SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM. |
- Theranostics, 2023, 13(10):3149-3164
- JCI Insight, 2023, 8(16)e170434
- JCI Insight, 2023, 8(16)e170434
|
|
S4259 |
Vilazodone HCl
|
Vilazodone HCl(EMD68843,SB659746A) is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder. |
- J Pain, 2019, 20(1):16.e1-16.e16
- Acta Pol Pharm, 2017, 74(3):765-775
|
|
S2096 |
Almotriptan Malate
|
Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. |
- Oncotarget, 2017, 9(3):3507-3518
- Oncotarget, 2016, 7(9):9975-92
|
|
S5401 |
Tegaserod Maleate
|
Tegaserod Maleate(HTF-919) is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors. |
- Cancers (Basel), 2022, 14(15)3592
- Front Oncol, 2021, 11:683241
|
|
S1432 |
Sumatriptan Succinate
|
Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches. |
- J Toxicol Sci, 2017, 42(6):755-761
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S1649 |
Zolmitriptan
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Zolmitriptan(BW-311C90) is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines. |
- Int J Pharm, 2019, 560:294-305
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S2852 |
BRL-54443
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BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. |
- bioRxiv, 2024, 10.1101/2024.01.28.577572
- Theranostics, 2021, 11(14):6950-6965
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S4256 |
Buspirone HCl
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Buspirone(Buspirone hydrochloride) is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. |
- Food Chem Toxicol, 2020, 30;141:111394
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S4751 |
Cisapride hydrate
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Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic. |
- Elife, 2021, 10e68714
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S1488 |
Naratriptan HCl
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Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches. |
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S1607 |
Rizatriptan Benzoate
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Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks. |
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S1385 |
Mosapride Citrate
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Mosapride Citrate (TAK-370, AS-4370, Gasmotin) is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
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S3180 |
Eletriptan HBr
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Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively. |
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S5741 |
Quetiapine
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Quetiapine(ICI204636) is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55. |
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S0496 |
PF-04995274
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PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. |
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S5848 |
Frovatriptan Succinate
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Frovatriptan Succinate(SB 209509 Succinate,VML 251 Succinate) is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors. |
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S5153 |
Tetrahydroberberine
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Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors. |
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S5253 |
Cisapride (R 51619)
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Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects. |
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S6324 |
5-Methoxytryptamine
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5-Methoxytryptamine (Mexamine, Methoxytryptamine) is a tryptamine derivative that acts as a full agonist at the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors. |
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E4835New |
Sumatriptan
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Sumatriptan (GR43175) is a selective agonist of 5-HT1D receptor, which is effectively used in the acute treatment of migraine. It causes a vasopressor response in the systemic and pulmonary arterial circulations and coronary artery vasoconstriction. |
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S3510 |
NLX-101
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NLX-101 (F-15599) is a highly selective 5-HT1A receptor biased agonist that mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors. |
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E4856New |
Rotigotine Hydrochloride
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Rotigotine Hydrochloride (N-0923 Hydrochloride) is a potent Agonist of dopamine receptor, with Ki values of 0.71 nM for dopamine D3 receptor, 4-15 nM for D2, D5, D4 receptors, and 83 nM for dopamine D1 receptor. It also acts as a partial agonist of the 5-HT1A receptor, and as an antagonist of the α2B-adrenergic receptor. |
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E4851New |
Tandospirone citrate
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Tandospirone citrate, is a potent, selective and a partial agonist of the 5-HT1A receptor. It exhibited good permeability in the intestine, with passive diffusion being the main mode of drug absorption, it also has anxiolytic effects and can be used in generalized anxiety disorder treatments. |
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S8447 |
8-OH-DPAT (8-Hydroxy-DPAT)
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8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous. |
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S5965 |
Urapidil
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Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist. |
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E4870New |
Naratriptan
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Naratriptan is an agonist of 5-hydroxytryptamine1B/D (5-HT1B/D) receptors, which reduces the frequency of cluster headache. |
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S0104 |
Pardoprunox (SLV-308) hydrochloride
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Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively. |
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S0113 |
Eptapirone
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Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.The affinity (pKi) of F11440 for 5-HT1A binding sites is 8.33.
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S4839 |
Mosapride
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Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
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S2025 |
Urapidil HCl
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Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. |
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E2356 |
Tandospirone
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Tandospirone (SM-3997), a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM, has anxiolytic and antidepressant activities. |
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S2578 |
1-Phenylbiguanide
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1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM. |
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