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The endocannabinoid system is a complex cell-signaling network through which endogenous cannabinoid ligands regulate cell function by interaction with CB 1 and CB 2 cannabinoid receptors, and with the novel cannabinoid receptor GPR55. CB 1 , CB 2 , and GPR55 are expressed by islet β-cells where they modulate insulin secretion. We have previously shown that administration of the putative CB 2 antagonist/inverse agonist JTE 907 to human islets did not affect the insulinotropic actions of CB 2 agonists and it unexpectedly stimulated insulin secretion on its own. In this study, we evaluated whether the lack of antagonism could be related to the ability of JTE 907 to act as a GPR55 agonist.

Direct Stimulatory Effects of the CB2 Ligand JTE 907 in Human and Mouse Islets