Cannabinoid Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Cannabinoid Receptor Products

Catalog No. Information Product Use Citations Product Validations
S5119

Olivetol

Olivetol (5-Pentylresorcinol, 5-n-Amylresorcinol) is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2.

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.

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.

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.

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.

S8033New

6-Iodopravadoline (AM630)

6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.

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.

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.

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.

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.

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.

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.

S8017

WIN 55, 212-2 mesylate

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.

S9048

(+)-Gallocatechin

(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.

Catalog No. Information Product Use Citations Product Validations
S5119

Olivetol

Olivetol (5-Pentylresorcinol, 5-n-Amylresorcinol) is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2.

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

S8033New

6-Iodopravadoline (AM630)

6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.

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.

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.

Catalog No. 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.

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.

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.

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.

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.

S8017

WIN 55, 212-2 mesylate

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.

Catalog No. Information Product Use Citations Product Validations
S9048

(+)-Gallocatechin

(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.

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