A potent and selective CB1 receptor agonist
Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.
参考文献:
[1].Pertwee, R.G. Pharmacology of cannabinoid receptor ligands Curr. Med. Chem. 6(8), 635-664 (1999).
[2].Hillard, C.J., Manna, S., Greenberg, M.J., et al. Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1) J. Pharmacol. Exp. Ther. 289(3), 1427-1433 (1999).
动态评分
0.0