CB2 选择性激动剂 | 拮抗剂

AM1241

AM-1241 is a selective cannabinoid CB2 receptor agonist with K_i of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.

6-Iodopravadoline (AM630)

6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.

GW842166X

GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

BML-190

BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with K_i of 435 nM, with 50-fold selectivity over CB1 receptor.

Bay 59-3074

Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties.

Rimonabant (SR141716)

Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.