SR144528

**SR144528** is a synthetic small molecule that acts as a highly potent and selective inverse agonist and antagonist at the cannabinoid receptor type 2 (CB2 receptor). It shows subnanomolar affinity for the rat spleen and cloned human CB2 receptors (Ki = 0.6 nM) and is about 700-fold less active at the CB1 receptor (Ki = 400 nM)[1][5][10]. It is orally active, does not demonstrate affinity for over 70 other receptors, ion channels, or enzymes, and is mainly used as a research tool for studying immune modulation and the role of the CB2 receptor in the endocannabinoid system[1][7]. At higher, micromolar concentrations, SR144528 may exhibit off-target immunomodulatory effects not mediated by CB2[3]. Developed for preclinical use, SR144528 is not approved for therapeutic application in humans[7].

Other names

5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptanyl]pyrazole-3-carboxamideN-[(1S)-Endo-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl]-5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)pyrazole-3-carboxamide