Iodopravadoline (AM630)

Description: Iodopravadoline, formerly known as AM630, is an inverse agonist at the human cannabinoid CB1 receptor. Iodopravadoline has been found to attenuate the ability of a number of cannabinoids to inhibit electrically-evoked twitches of the mouse isolated vas deferens. AM630 was markedly more potent as an antagonist of delta 9-THC and CP 55, 940 (Kd = 14.0 and 17.3 nM respectively) than as an antagonist of WIN 55, 212-2, AM356 or anandamide (Kd = 36.5, 85.9 and 278.8 nM respectively).

References: Patil M, Patwardhan A, Salas MM, Hargreaves KM, Akopian AN. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology. 2011 Sep; 61(4):778-88. doi: 10.1016/j.neuropharm.2011.05.024. Epub 2011 May 27. PubMed PMID: 21645531; PubMed Central PMCID: PMC3130079.