Background
CAY10429-d3 contains three deuterium atoms at the terminal methyl position. It is intended for use as an internal standard for the quantification of CAY10429 by GC- or LC-mass spectrometry. Traditionally, the activity of cannabinoid (CB) agonists was thought to be transduced by a pair of G protein-coupled receptors, CB1 and CB2.1 CAY10429 (abnormal cannabidiol) is a synthetic regioisomer of cannabidiol that fails to elicit either CB1 or CB2 responsiveness and is without psychotropic activity. CAY10429 induces endothelium-dependent vasodilation via a CB1/CB2/nitric oxide-independent mechanism.2 At a dose of 20 µg/g in rats, CAY10429 showed hypotensive activity that could not be antagonized by cannabidiol or SR141716A. CAY10429 is therefore believed to activate a third type of CB receptor, provisionally called the non-CB1/CB2 endocannabinoid receptor. CAY10429 also acts via these receptors to regulate the migratory activity of murine BV-2 microglial cells, with an EC50 value of 600 nM.3
1.Felder, C.C., Joyce, K.E., Briley, E.M., et al.Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptorsMol. Pharmacol.48(3)443-450(1995)
2.Járai, Z., Wagner, J.A., Varga, K., et al.Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptorsProc. Natl. Acad. Sci. U.S.A.96(24)14136-14141(1999)
3.Walter, L., Franklin, A., Witting, A., et al.Nonpsychotropic cannabinoid receptors regulate microglial cell migrationJournal of Neuroscience23(4)1398-1405(2003)
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