cb1r

CB1R Allosteric modulator 3 is a potent CB1R modulator that inhibits cAMP and β-Arrestin and can be used for the study of obesity and nicotine addiction.

CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system.

Drinabant (AVE-1625) is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.

CB1R antagonist 2 (Compound 11g) functions as an antagonist of the cannabinoid receptor 1 (CB1R), inhibiting the MAPK NF-κB signaling pathway and exhibiting anti-inflammatory properties. In RAW264.7 cells, it suppresses LPS-induced expression of IL-6, IL-1β, and TNF-α. In murine models, it improves OVA-induced allergic rhinitis.

CB1R Allosteric Modulator 2 (compound 18) is a potent negative allosteric modulator (NAM) of CB1R receptor activity, as demonstrated in previous studies [1].

CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].

CB1R Allosteric Modulator 1 (compound 11) is a potent allosteric modulator of CB1Rs, negatively affecting the functional activity of orthosteric ligands [NAM] at CB1Rs.

Compound 38-S is an orally active CB1R AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [1].

NESS 0327 is a high selectivity antagonist of the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor.

CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and > 1000 nM for CB2 and CB1 receptors respectively.

JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.

CB2R FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

Taranabant (MK-0364) is a selective and potent cannabinoid 1 (CB1) receptor inverse agonist used in the study of obesity and nicotine dependence.

O-1269 acts as a partial agonist for the cannabinoid receptor 1 (CB1R), with a binding affinity (Ki) of 32 nM. Additionally, it exhibits analgesic properties.

AM6545 is a selective and potent peripheral restricted cannabinoid receptor 1 (CB1) antagonist that inhibits the CB2 receptor, ameliorates hypometabolic obesity and improves adipokine secretion in monosodium glutamate-induced obese mice, and may be useful in the study of obesity and diabetes.

MJ 15 is a CB1 receptor antagonist with specificity for the study of obesity-induced diseases.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a potent and selective antagonist of cannabinoid receptor type 1 (CB1R) and inducible nitric oxide synthase (iNOS), with a binding affinity (Ki) of 5.7 nM for CB1R. It holds promise as an investigative tool in liver fibrosis research due to these characteristics.

GAT564 (Compound 15d) is a highly effective allosteric modulator of the cannabinoid 1 receptor (CB1R), with EC50 values of 87 nM for cAMP and 320 nM for β-arrestin2. It significantly enhances the binding of orthosteric ligands to hCB1R and exhibits remarkable efficacy as a topical agent, significantly reducing intraocular pressure (IOP) in an ocular normotensive murine model of glaucoma [1].

CB1 2 agonist 1 is a potent CB1 2 agonist that crosses the blood-brain barrier, acting on CB1R (EC50: 56.15 nM) and CB2R (EC50: 11.63 nM). It reduces glutamate release and LPS-induced microglia activation, exhibiting anti-inflammatory and analgesic activities, with potential for multiple sclerosis studies.

CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist that targets CB1R with a Ki of 0.18 μM and CB2R with a Ki of 1.22 μM. It can be utilized to investigate diseases related to the endogenous cannabinoid system.

CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC50 of 960 nM and Ki of 970 nM, making it a promising tool for studying diseases related to the endogenous cannabinoid system involving hCB1R.