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Cannabinoid Receptor

Isoform-selective Products

Signaling Pathway

Cannabinoid Receptor Signaling Pathway

Cannabinoid Receptor Products

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  • Cannabinoid Receptor Inhibitor (1)
  • Cannabinoid Receptor Antibodies (2)
  • Cannabinoid Receptor Activator (1)
  • Cannabinoid Receptor Antagonists (7)
  • Cannabinoid Receptor Agonists (7)
  • Cannabinoid Receptor Modulators (2)
  • New Cannabinoid Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
Brain Behav Immun, 2023, 110:60-79
Asian J Pharm Sci, 2023, 18(4):100835
Asian J Pharm Sci, 2023, 18(4):100835
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Pharmacol Res, 2023, 194:106864
Physiol Rep, 2023, 11(1):e15565
Sci Rep, 2021, 11(1):11515
S3021 Rimonabant (SR141716) Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
Mol Metab, 2022, 65:101597
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
Nat Commun, 2020, 11(1):71
Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
S2854 BML-190 BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Int J Mol Sci, 2020, 21(7)
University of Alberta, 2014, Yahya Muhammad Fiteih
S8033 6-Iodopravadoline (AM630) 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.
Brain Behav Immun, 2023, 110:60-79
Pharmacol Res, 2023, 194:106864
S2778 GW842166X GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
Nat Commun, 2020, 11(1):71
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.
Biochem Pharmacol, 2024, 224:116190
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
E4945New Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC).
E0458 RTICBM-189 RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.
E1841New Monlunabant Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.
E4585New N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells.
E4858New Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors.
S9048 (+)-Gallocatechin (+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.
S0412 Bay 59-3074 Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties.
S9413 Yangonin Yangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors.
S8694 CID16020046 CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Pharmacol Res, 2024, 203:107176
A2574 Nimacimab (Anti-CB1 / CNR1) Nimacimab (Anti-CB1/CNR1) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases. MW:145.5 KD.
A2575 Anti-CB1 / CNR1 Anti-CB1 / CNR1 (GFB-024) is a recombinant humanised monoclonal antinody that is used for targeting of CB1 receptor. MW:145.5 KD.
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor.
E4945New Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC).
A2574 Nimacimab (Anti-CB1 / CNR1) Nimacimab (Anti-CB1/CNR1) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases. MW:145.5 KD.
A2575 Anti-CB1 / CNR1 Anti-CB1 / CNR1 (GFB-024) is a recombinant humanised monoclonal antinody that is used for targeting of CB1 receptor. MW:145.5 KD.
S9413 Yangonin Yangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors.
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Pharmacol Res, 2023, 194:106864
Physiol Rep, 2023, 11(1):e15565
Sci Rep, 2021, 11(1):11515
S3021 Rimonabant (SR141716) Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
Mol Metab, 2022, 65:101597
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
Nat Commun, 2020, 11(1):71
Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
S8033 6-Iodopravadoline (AM630) 6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.
Brain Behav Immun, 2023, 110:60-79
Pharmacol Res, 2023, 194:106864
E4858New Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors.
S8694 CID16020046 CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Pharmacol Res, 2024, 203:107176
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor.
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
Brain Behav Immun, 2023, 110:60-79
Asian J Pharm Sci, 2023, 18(4):100835
Asian J Pharm Sci, 2023, 18(4):100835
S2854 BML-190 BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Int J Mol Sci, 2020, 21(7)
University of Alberta, 2014, Yahya Muhammad Fiteih
S2778 GW842166X GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
Nat Commun, 2020, 11(1):71
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.
Biochem Pharmacol, 2024, 224:116190
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
E1841New Monlunabant Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.
E4585New N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells.
S0412 Bay 59-3074 Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties.
E0458 RTICBM-189 RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.
S9048 (+)-Gallocatechin (+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.
E4945New Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC).
E1841New Monlunabant Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.
E4585New N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells.
E4858New Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors.

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Tags: Cannabinoid Receptor signaling | CB1 receptor signaling | CB2 signaling | Cannabinoid Receptor inhibitor review