Add time:07/15/2019         Source:sciencedirect.com

The aminoalkylindole BML-190 (cas 2854-32-2) and diarylpyrazole AM251 ligands have previously been shown to bind to cannabinoid CB2 and CB1 receptors, respectively. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 and AM251 potentiated the forskolin-stimulated accumulation of cAMP. Moreover, the CB2 receptor can interact productively with 16z44, a promiscuous Gα16/z chimera. BML-190 and AM251 reduce the basal levels of inositol phosphate production in cells expressing the CB2 receptor and 16z44. These results demonstrate that BML-190 and AM251 act as inverse agonists at the human CB2 receptor acting via Gαi/o and Gαq family-coupled pathways.

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