AM630 (Synonyms: 6-Iodopravodoline)

AM630 is a selective and competitive antagonist of cannabinoid receptors with Ki values of 5 μM and 31.2 nM for CB1 receptor and CB2 receptor, respectively [1].

In CB1-transfected CHO cells, AM630 significantly inhibited the production of cAMP stumilated by forskolin. In CB2-transfected cells, AM630 promoted forskolin to stimulate cyclic AMP production with EC50 value of 230.4 nM. AM630 also exerted to have inhibitory effect on the binding of GTPγS to membranes from CB2-transfected cells. Besides that, AM630 was found to activate the TRPA1 channels and subsequently desensitizing TRPA1 and TRPV1 channels in TG sensory neurons. Moreover, AM630 significantly weakened the thermal hyperalgesia induced by CAP (capsaicin) in WT mice [1, 2].

References:
1. Ross R A, Brockie H C, Stevenson L A, et al. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. British journal of pharmacology, 1999, 126(3): 665-672.
2. Patil M, Patwardhan A, Salas M M, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788.