A potent and selective CB1 receptor agonist
Arachidonoyl cyclopropylamide (ACPA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 2.2 and 715 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACPA 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:
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[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).
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