Signaling Pathway

Cannabinoid Receptor

Cannabinoid Receptor

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Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.

Cannabinoid Receptor Inhibitors & Modulators (16)

Product Name Catalog No. Brief Description
A-836339

HY-12761

A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.

AM251

HY-15443

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).

AM630

HY-15421

AM630 is a selectivity CB2 antagonist with Ki of 31.2 nM; > 150 fold selectivity over CB1 receptor.

Bay 59-3074

HY-100488

Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively .

BML-190

HY-15420

BML-190(IMMA) is a potent and selective CB2 receptor ligand (Ki values are 435 nM and > 2 μM for CB2 and CB1 respectively).

CB1-IN-1

HY-12790

CB1-IN-1 is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.

JWH-133

HY-15854

JWH 133 is a potent CB2 selective agonist with Ki of 3.4 nM, 200-fold selective over CB1 receptors.

MDA 19

HY-15451

MDA 19 is a selective human CB2 receptor agonist with Ki of 43.3 nM.

Org 27569

HY-13288

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.

Otenabant

HY-10871

Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.

Otenabant Hydrochloride

HY-10871A

Otenabant Hcl (CP-945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.

Rimonabant

HY-14136

Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

Rimonabant Hydrochloride

HY-14137

Rimonabant Hcl(SR141716A) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

Taranabant

HY-10013

Taranabant(MK 0364) is a cannabinoid 1 receptor inverse agonist with IC50 of 0.3 nM.

Taranabant (1R,2R)stereoisomer

HY-10013B

Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant.

WIN 55,212-2 Mesylate

HY-13291

(+)WIN 55212-2 mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.