In vitro metabolism of indomethacin morpholinylamide (BML-190 (cas 2854-32-2)), an inverse agonist for the peripheral cannabinoid receptor (CB2) in rat liver microsomes

Add time:07/16/2019    Source:sciencedirect.com

The in vitro metabolism of an inverse agonist of the peripheral cannabinoid receptor (CB2), indomethacin morpholinylamide (BML-190), has been characterized using rat liver microsomal incubation. BML-190 was found to yield at least 15 metabolic products as identified by HPLC–MS/MS analysis. Four major phase one metabolic pathways either individually, or in combination, were proposed to account for the identified metabolic products: (1) loss of the p-chlorobenzyl group, (2) hydroxylation on the indole or on the morpholine ring, (3) morpholinyl ring opening, and (4) demethylation of the methoxyl group on the indole ring.

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