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GPCR/G Protein Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid receptors are of a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids, produced by the mammillary body;[citation needed] plant cannabinoids (such as cannabidiol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and phytocannabinoids (plant based cannabinoids) are lipophilic, such as fat soluble compounds.
Cat No. product name
T1519 Rimonabant hydrochloride Rimonabant hydrochloride is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.
T1519L Rimonabant Rimonabant is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue...
T1796 Otenabant hydrochloride Otenabant hydrochloride (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).
T1915 AM251 AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 ...
T2264 AM281 AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.
T2635 Org 27569 Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and ...
T3699 Bay 59-3074 Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic...
T6417 BML-190 BML-190 is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor.
T6527 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...
T9114 β-Caryophyllene β-Caryophyllene is a CB2 receptor agonist.
T4654 SLV319 SLV319 has been used in trials studying the treatment of Obesity and Obesity and Type 2 Diabetes.
T3530 Otenabant Otenabant has been investigated for the treatment of Obesity.
TWS0414 Cannabidiol Cannabidiol is GPR55 and weak CB1 antagonist (IC50s: 0.445 and 3.35 μM), CB2 receptor inverse agonist and inhibitor of anandamide uptake (IC50: 27.5 μM). It a...
T5996 CB1-IN-1 CB1-IN-1 is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.
T7316 LY2828360 LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM...
T7375 A-836339 A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 rece...
T7705 GW 405833 GW 405833 is an agonist of cannabinoid-2 (CB(2)) receptor-selective 
TQ0173 MDA 19 MDA 19 is a specific human CB2 receptor agonist (Ki: 43.3 nM).
T4453 JD-5037 JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
T3S0738 yangonin 1. Yangonin exhibits affinity for the human recombinant CB₁ receptor. 2. Yangonin could be a valuable candidate for the intervention of NF-κB-dependent p...
TN2268 Tetrahydromagnolol Tetrahydromagnolol can activate cannabinoid (CB) receptors.
T14204 6-Iodopravadoline 6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.
T14302 Olorinab Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.
T14504 BAY 38-7271 BAY 38-7271 has strong neuroprotective properties.[1] BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist. With Kis of 1.85 nM a...
T13081 Taranabant racemate Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor.
T10510 CB1 antagonist 1 CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gas...
T10694 CB1 inverse agonist 1 CB1 inverse agonist 1 is an orally active, and specific inverse agonist of the CB1 receptor (IC50s: 7.5 nM and 4100 nM for CB1 and CB2 receptors) with anorexige...
T17104 TM38837 TM38837 is a peripheral selective cannabinoid receptor type 1 receptor antagonist. TM38837 decreases the propensity for psychiatric side effects. TM38837 displa...
T16928 SR144528 SR144528 is an effective and selective antagonist of the CB2 receptor (Ki: 0.6 nM).
T17027 Tedalinab Tedalinab is an effective and selective cannabinoid receptor 2 agonist. Tedalinab has the potential for neuropathic pain and osteoarthritis treatment. Tedalinab...
TN5131 Tetrahydrocannabivarin Tetrahydrocannabivarin is a neutral cannabis receptor subtype (CB1) receptor antagonist, it can increases neural responding to rewarding and aversive stimuli, t...
Rimonabant hydrochloride
T1519CAS 158681-13-1
Rimonabant hydrochloride is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.
Rimonabant
T1519LCAS 168273-06-1
Rimonabant is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue...
Otenabant hydrochloride
T1796CAS 686347-12-6
Otenabant hydrochloride (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).
AM251
T1915CAS 183232-66-8
AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 ...
AM281
T2264CAS 202463-68-1
AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.
Org 27569
T2635CAS 868273-06-7
Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and ...
Bay 59-3074
T3699CAS 406205-74-1
Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic...
BML-190
T6417CAS 2854-32-2
BML-190 is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor.
GW842166X
T6527CAS 666260-75-9
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...
β-Caryophyllene
T9114CAS 87-44-5
β-Caryophyllene is a CB2 receptor agonist.
SLV319
T4654CAS 362519-49-1
SLV319 has been used in trials studying the treatment of Obesity and Obesity and Type 2 Diabetes.
Otenabant
T3530CAS 686344-29-6
Otenabant has been investigated for the treatment of Obesity.
Cannabidiol
TWS0414CAS 13956-29-1
Cannabidiol is GPR55 and weak CB1 antagonist (IC50s: 0.445 and 3.35 μM), CB2 receptor inverse agonist and inhibitor of anandamide uptake (IC50: 27.5 μM). It a...
CB1-IN-1
T5996CAS 1429239-98-4
CB1-IN-1 is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.
LY2828360
T7316CAS 1231220-79-3
LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM...
A-836339
T7375CAS 959746-77-1
A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 rece...
GW 405833
T7705CAS 180002-83-9
GW 405833 is an agonist of cannabinoid-2 (CB(2)) receptor-selective 
MDA 19
TQ0173CAS 1048973-47-2
MDA 19 is a specific human CB2 receptor agonist (Ki: 43.3 nM).
JD-5037
T4453CAS 1392116-14-1
JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
yangonin
T3S0738CAS 500-62-9
1. Yangonin exhibits affinity for the human recombinant CB₁ receptor. 2. Yangonin could be a valuable candidate for the intervention of NF-κB-dependent p...
Tetrahydromagnolol
TN2268CAS 20601-85-8
Tetrahydromagnolol can activate cannabinoid (CB) receptors.
6-Iodopravadoline
T14204CAS 164178-33-0
6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.
Olorinab
T14302CAS 1268881-20-4
Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.
BAY 38-7271
T14504CAS 212188-60-8
BAY 38-7271 has strong neuroprotective properties.[1] BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist. With Kis of 1.85 nM a...
Taranabant racemate
T13081CAS 701977-00-6
Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor.
CB1 antagonist 1
T10510CAS 890037-68-0
CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gas...
CB1 inverse agonist 1
T10694CAS 852315-00-5
CB1 inverse agonist 1 is an orally active, and specific inverse agonist of the CB1 receptor (IC50s: 7.5 nM and 4100 nM for CB1 and CB2 receptors) with anorexige...
TM38837
T17104CAS 1253641-65-4
TM38837 is a peripheral selective cannabinoid receptor type 1 receptor antagonist. TM38837 decreases the propensity for psychiatric side effects. TM38837 displa...
SR144528
T16928CAS 192703-06-3
SR144528 is an effective and selective antagonist of the CB2 receptor (Ki: 0.6 nM).
Tedalinab
T17027CAS 916591-01-0
Tedalinab is an effective and selective cannabinoid receptor 2 agonist. Tedalinab has the potential for neuropathic pain and osteoarthritis treatment. Tedalinab...
Tetrahydrocannabivarin
TN5131CAS 31262-37-0
Tetrahydrocannabivarin is a neutral cannabis receptor subtype (CB1) receptor antagonist, it can increases neural responding to rewarding and aversive stimuli, t...