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.

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].

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

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

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.

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.

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.

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.

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

CB2R FAAH modulator-3 (compound 27) is a modulator targeting CB2R and FAAH, acting as a CB2R agonist with a Ki value of 20.1 nM and a CB1R agonist with a Ki value of 67.6 nM, while inhibiting FAAH with an IC50 value of 3.4 μM. This compound has research value in cancer, neurodegenerative disease-related inflammatory cascades, and COVID-19 infection.

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.

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

(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.

GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs.

CB2R FAAH modulator-2 (compound 26) is a dual modulator targeting CB2R and FAAH, acting as a CB2R agonist (Ki = 10.8 nM) and FAAH inhibitor (IC50 = 6.2 μM), with a Ki value of 152.9 nM for CB1R. It has research value in cancer, deleterious inflammatory cascades in neurodegenerative diseases, and COVID-19 infection.

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

CB2R-IN-3 is a selective antagonist of cannabinoid type 2 receptor (CB2R) . CB2R-IN-3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R-IN-3 can be combined with CB65 , the activator of CB2R. CB2R-IN-3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines [1] .

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.

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.

AEF0117, a signaling-specific inhibitor of cannabinoid receptor 1 (CB1-SSi), inhibits cannabinoid self-administration and behavioral disorders associated with THC, and can be used to study cannabis withdrawal.