cb2r

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.

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.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

Compound 2o, also known as CB2R 5-HT1AR agonist 1, serves as a partial orally active agonist for the CB2 receptor (EC50 = 479.6 nM) and a full agonist for the 5-HT1A receptor (EC50 = 2.7 μM). This compound demonstrates both anti-anxiety and anti-depressive effects and has favorable pharmacokinetic properties [1].

CB2R Probe 1, a cannabinoid 2 receptor (CB2R) fluorescent probe, exhibits both safety and environmental friendliness, boasting a dissociation constant (K i) of 130 nM. Notably, it demonstrates low cytotoxicity within cancer cells [1].

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] .

CB2R PAM is an orally active cannabinoid type 2 receptor (CB2Rs) positive allosteric modulator that enhances CP 55940 and 2-Arachidonylglycerol-stimulated [35S]GTPγS binding to CB2 receptors without affecting receptor activity in the absence of agonists. CB2R PAM shows anti-injury activity in a mouse model of neuropathic pain.

CB2R agonist 2 (cis-17-para) is a CB2R agonist [1].

CB2R agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [1].

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

CB2R agonist 1, a selective ligand for the cannabinoid receptor subtype 2 (CB2R), demonstrates a high affinity and excellent selectivity, with an EC50 value of 0.56 µM, favoring human CB2R over CB1R. It plays an immunomodulatory role by regulating the production of both pro-inflammatory and anti-inflammatory cytokines.

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.

hBChE-IN-2 is a butyrylcholinesterase (BChE) inhibitor and cannabinoid receptor 2 (CB2R) agonist with neuroprotective activity for the study of Alzheimer's disease-like neurological disorders.

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.

PGN36 (Compound 18) is a potent and highly selective antagonist of the cannabinoid CB2 receptor (CB2R), exhibiting exceptional affinity with a Ki value of 0.09 μM [1].

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.

RNB-61 is an orally active cannabinoid CB2 receptor (CB2R) agonist, displaying a Ki range between 0.13 nM and 1.81 nM. It possesses renal protective and or anti-fibrotic properties. Additionally, the permeability of RNB-61 into the brain is negligible.

Arachidonylcyclopropylamide (AM1241) is a highly effective and selective agonist for the CB2R. This compound specifically targets the CB2 receptor, making it a valuable tool for research and therapeutic applications that exploit CB2-specific pathways without affecting CB1 receptors.

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.

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.