CAY10429-d3

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)