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.

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.

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

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.

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.

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 agonist 1 (Compound '1350) is a potent full agonist of the cannabinoid-1 receptor (CB1R) with a Ki value of 0.95 nM. It demonstrates significant pain-relieving effects in various pain models, including acute thermal pain, inflammatory pain, and neuropathic pain.

CB1R Allosteric modulator 5 (compound 3) is a selective allosteric modulator of cannabinoid receptor type 1 (Cannabinoid receptor type 1) that can cross the blood-brain barrier, with a pIC0 value of 6.89. It reduces cue-induced reinstatement of cocaine-seeking behavior and cocaine-induced behavioral sensitization without altering motor activity.

PROTACCB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that employs the ubiquitin-proteasome system (UPS) to facilitate CB1R degradation, showing a DC50 of 3.37 μM in MCF-7 cells while exhibiting no effect on CB2R. It reduces CB1R-associated downstream signaling pathways (p-AKT, p-ERK, BCL2, and MCM5), thus inhibiting breast cancer cell proliferation and inducing apoptosis. PROTACCB1R Degrader-1 is applicable for breast cancer-related research.

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].

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies.

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

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.

CB1 antagonist6 (Compound 11jE2) is an orally active CB1R antagonist with an IC50 value of 23 nM. It significantly reduces food intake and body weight in diet-induced obesity (DIO) mice, improves glucose tolerance and insulin resistance, and lowers serum ALT and AST levels, demonstrating hepatoprotective effects. CB1 antagonist6 is applicable for studies on metabolic syndrome, including obesity and diabetes.