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GABA Receptor Signaling Pathway

GABA Receptor Products

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  • GABA Receptor Inhibitors (11)
  • GABA Receptor Activators (7)
  • GABA Receptor Antagonists (14)
  • GABA Receptor Agonists (15)
  • GABA Receptor Modulators (10)
  • New GABA Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Exp Med, 2022, 219-12e20220541
Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7
S6611 Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.
Nucleic Acids Res, 2024, gkae761
Adv Sci (Weinh), 2023, 10(3):e2203718
iScience, 2022, 25-9:104952
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.
Front Pharmacol, 2022, 13:932092
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
S2133 Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Oncol, 2022, 10.1002/1878-0261.13281
Mol Pharmacol, 2022, 101(4):236-245
Cell Death Dis, 2020, 11(9):764
S1332 Flumazenil Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
J Exp Med, 2022, 219-12e20220541
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S1338 Gabapentin HCl Gabapentin HCl(Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
S0303 CGP52432 CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
S3072 (R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
J Cell Biochem, 2022, 10.1002/jcb.30231
S3018 Niflumic acid Niflumic acid(Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
S2026 Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Cell Rep, 2020, 21;31(3):107521
S5194 Furosemide sodium Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.
Nat Commun, 2024, 15(1):7342
Ren Fail, 2022, 44(1):1345-1355
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Life Sci, 2021, S0024-3205(20)31752-5
S4700 4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid) is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
Theranostics, 2023, 13(4):1355-1369
S1969 Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
E1247 SR95531 Gabazine(SR95531) is a potent competitive and allosteric antagonist of the GABAA receptor, with an IC50 for the GABA receptor of 9 µM.
E3045 Chinese Arborvilea Seed Extract Chinese Arborvilea Seed Extract is extracted from the dried and mature seed kernels of Platycladus orientalis (L.)Franco, has obvious anti-anxiety effect, and its mechanism may be related to increasing GABA level and decreasing Glu level in hippocampus.
E2848 Afoxolaner Afoxolaner (NexGard) is a new insecticide/acaricide molecule from the isoxazoline family that acts on the insect gamma-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
S5131 Homotaurine Homotaurine (Tramiprosate, Alzhemed, 3-Amino-1-propanesulfonic acid) is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S3959 (+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S4840 Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
S2996 L-DAB HBR

L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity.
S3634 6-Hydroxyflavone (6-HF) 6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors.
E2354 Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S5596 (1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
S9249 Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S4892 Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
S4587 Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ) displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
Cell Mol Life Sci, 2024, 81(1):104
E3607 Crateva nurvala Extract Crateva Nurvala Extract is extracted from the stem bark of Crataeva nurvala Buch.. Crateva nurvala, an important medicinal plant, has been studied mainly with the stem bark part for obstructive and nonobstructive uropathies. Crateva nurvala is also used for the treatment of prostate enlargement and bladder sensitivity.
E0599 Arecaidine hydrochloride Arecaidine hydrochloride, a constituent of the nut of Areca catechu, inhibits the uptake of GABA and beta-alanine, but not that of glycine.
E0101 AZD6280 AZD6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
S4961 3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
E4920New Baclofen hydrochloride Baclofen hydrochloride is an agonist of the GABAB receptor that mimics the action of GABA, leading to slow presynaptic inhibition via the GABAB receptor. It improves the function of the ubiquitin-proteasome system (UPS) and enhances cell survival in both in vitro and in vivo models of Huntington's disease (HD).
S4661 Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S3663 Afloqualone Afloqualone (AFQ, HQ-495) is a quinazolinone family GABAergic drug with muscle-relaxant and sedative effects, showing the agonist activity at the β subtype of the GABAa receptor.
S4675 Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S6008 p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. p-Hydroxybenzaldehyde at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed.
S9065 Songorine Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.
S1989 GABAA receptor agent 1 GABAA receptor agent 1 is a high affinity ligand for Gamma-aminobutyric acid A (GABAA) receptor that exerts potent anticonvulsant activity.
S4197 Bemegride Bemegride(Bemegrid,3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
S5049 Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
S4270 Oxiracetam Oxiracetam (ISF 2522), a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
Eur J Pharmacol, 2024, 979:176835
S0164 AZD7325 AZD7325 is a potent and orally active partial selective Positive allosteric modulator (PAM) of GABAAα2 and Aα3 receptor with Ki=0.3 and 1.3 nM, respectively, and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes.
S9409 Kavain Kavain ((+)-Kavain), the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.
E2232 Guvacine hydrochloride Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and displays modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
S4772 alpha-Asarone Alpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects.
S5319 Imepitoin Imepitoin(ELB-138,AWD 131-138) is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
S6100 Picrotoxin Picrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139), a plant alkaloid, is a non-competitive antagonist of neuronal GABA and glycine receptors.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate,N-acetylhomotaurinate) is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S6470 Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
S3977 (-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
S4494 Methionine Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity.
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
E3508 Magnolia Obovata Extract Magnolia Obovata Extract is extracted from magnolia obovata, which has an anxiolytic effect through enhancement of the GABA receptor and anti-neuroinflammatory mechanisms.
S5612 Isonipecotic acid Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
E0960 RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
S3018 Niflumic acid Niflumic acid(Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
E1247 SR95531 Gabazine(SR95531) is a potent competitive and allosteric antagonist of the GABAA receptor, with an IC50 for the GABA receptor of 9 µM.
E2848 Afoxolaner Afoxolaner (NexGard) is a new insecticide/acaricide molecule from the isoxazoline family that acts on the insect gamma-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
S2996 L-DAB HBR

L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity.
E0599 Arecaidine hydrochloride Arecaidine hydrochloride, a constituent of the nut of Areca catechu, inhibits the uptake of GABA and beta-alanine, but not that of glycine.
S4661 Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S4675 Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
E2232 Guvacine hydrochloride Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and displays modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
S6470 Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
E3508 Magnolia Obovata Extract Magnolia Obovata Extract is extracted from magnolia obovata, which has an anxiolytic effect through enhancement of the GABA receptor and anti-neuroinflammatory mechanisms.
S1969 Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
E3045 Chinese Arborvilea Seed Extract Chinese Arborvilea Seed Extract is extracted from the dried and mature seed kernels of Platycladus orientalis (L.)Franco, has obvious anti-anxiety effect, and its mechanism may be related to increasing GABA level and decreasing Glu level in hippocampus.
E2354 Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S4772 alpha-Asarone Alpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects.
S5319 Imepitoin Imepitoin(ELB-138,AWD 131-138) is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4494 Methionine Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity.
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Exp Med, 2022, 219-12e20220541
Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7
S1332 Flumazenil Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
J Exp Med, 2022, 219-12e20220541
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S0303 CGP52432 CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
S2026 Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Cell Rep, 2020, 21;31(3):107521
S5194 Furosemide sodium Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.
Nat Commun, 2024, 15(1):7342
Ren Fail, 2022, 44(1):1345-1355
S9249 Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S4587 Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ) displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
Cell Mol Life Sci, 2024, 81(1):104
S6008 p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. p-Hydroxybenzaldehyde at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed.
S9065 Songorine Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.
S4197 Bemegride Bemegride(Bemegrid,3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
S5049 Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.
S6100 Picrotoxin Picrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139), a plant alkaloid, is a non-competitive antagonist of neuronal GABA and glycine receptors.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.
Front Pharmacol, 2022, 13:932092
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
S2133 Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Oncol, 2022, 10.1002/1878-0261.13281
Mol Pharmacol, 2022, 101(4):236-245
Cell Death Dis, 2020, 11(9):764
S1338 Gabapentin HCl Gabapentin HCl(Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
S3072 (R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
J Cell Biochem, 2022, 10.1002/jcb.30231
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Life Sci, 2021, S0024-3205(20)31752-5
S4700 4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid) is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
Theranostics, 2023, 13(4):1355-1369
S4840 Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
S3634 6-Hydroxyflavone (6-HF) 6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors.
S4892 Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
S4961 3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
E4920New Baclofen hydrochloride Baclofen hydrochloride is an agonist of the GABAB receptor that mimics the action of GABA, leading to slow presynaptic inhibition via the GABAB receptor. It improves the function of the ubiquitin-proteasome system (UPS) and enhances cell survival in both in vitro and in vivo models of Huntington's disease (HD).
S3663 Afloqualone Afloqualone (AFQ, HQ-495) is a quinazolinone family GABAergic drug with muscle-relaxant and sedative effects, showing the agonist activity at the β subtype of the GABAa receptor.
S4270 Oxiracetam Oxiracetam (ISF 2522), a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
Eur J Pharmacol, 2024, 979:176835
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate,N-acetylhomotaurinate) is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S5612 Isonipecotic acid Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.
S6611 Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.
Nucleic Acids Res, 2024, gkae761
Adv Sci (Weinh), 2023, 10(3):e2203718
iScience, 2022, 25-9:104952
S5131 Homotaurine Homotaurine (Tramiprosate, Alzhemed, 3-Amino-1-propanesulfonic acid) is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S3959 (+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S5596 (1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
E0101 AZD6280 AZD6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
S0164 AZD7325 AZD7325 is a potent and orally active partial selective Positive allosteric modulator (PAM) of GABAAα2 and Aα3 receptor with Ki=0.3 and 1.3 nM, respectively, and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes.
S9409 Kavain Kavain ((+)-Kavain), the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
S3977 (-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
E0960 RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.
E4920New Baclofen hydrochloride Baclofen hydrochloride is an agonist of the GABAB receptor that mimics the action of GABA, leading to slow presynaptic inhibition via the GABAB receptor. It improves the function of the ubiquitin-proteasome system (UPS) and enhances cell survival in both in vitro and in vivo models of Huntington's disease (HD).

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