cb2 receptor

SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

CB2 receptor antagonist 4 is a selective inverse agonist for the CB2 receptor with a Kd value of 39 nM.

GP 2A is a selective agonist of CB2 receptor.

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

CB2receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R, with a binding affinity (Kd) of 39 nM. This compound serves as a tool for synthesizing various CB2R probes.

CB2receptor agonist 6 (compound 70) is a CB2R agonist with an EC50 of 162 nM. It has IC50 values of 4.83 μM for CB1R and 0.88 μM for CB2R. As a neuroprotective agent, CB2receptor agonist 6 is useful for research in neurological disorders.

CB2receptor agonist 4 (Compound 8) is a highly selective agonist for the cannabinoid type 2 receptor (CB2Receptor), with an EC50 of 13.99 nM. This compound exhibits no significant activity on the type 1 cannabinoid receptor. It is useful for researching pain and immune-related diseases.

Hexyl resorcinol derivative 29 is a CB2 selective competitive antagonist/reverse agonist demonstrating notable potency. Meanwhile, Olivanol and 5-(2-methyloctane-2-yl) resorcinol derivatives 23 and 24 exhibit substantial antinociceptive effects. Notably, compound 24 activates both cannabinoid and TRPV1 receptors.

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.

GW 833972A is a selective CB2 receptor agonist that inhibits induced neural depolarization and citric acid-induced cough in an animal model.

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.

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.

CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. It can induce apoptosis, promote reactive oxygen species (ROS) production, and cause protein misfolding. Additionally, CB2R agonist 4 exhibits cytotoxicity against various tumor cells and is applicable for cancer research.

ISAM-CG557 is a selective CB2R agonist with a Ki of 54.6 nM. It reduces intracellular ROS levels and caspase activity, demonstrating significant MAPK bias and moderate G-protein bias, with CB2REC50 values of 0.60 nM for cAMP, 60.9 nM for β-arrestin, and 0.03 nM for MAPK. ISAM-CG557 exerts potent anti-inflammatory effects by decreasing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. It is utilized in the study of neuroinflammation and neurodegenerative diseases.

CB2R antagonist 4 is a selective CB2R antagonist/inverse agonist with a pKi value of 6.54. It demonstrates at least 11 times greater selectivity for CB2R over CB1R and can be utilized in neuroscience research.

VU6077967 is a selective agonist for the cannabinoid receptor 2 (CB2), exhibiting an EC50 of 8.6 nM for rCB2. It is suitable for research into neurological disorders, including Alzheimer's disease.

AZD1940 (UNII-0J0035E9FT) is a high affinity CB(1)/CB(2) receptor agonist of the cannabinoid with oral activity. Application in the study of orofacial pain.

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

CB1/2 agonist 3 is a competitive and potent CB1/CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki values of 3.5 nM and 1.2 nM, respectively. It acts as a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 shares these properties, being a complete agonist of CB1 and a competitive inverse agonist of CB2.

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.