title: In vitro metabolism of indomethacin morpholinylamide (BML-190), an inverse agonist for the peripheral cannabinoid receptor (CB(2)) in rat liver microsomes.
abstract: The in vitro metabolism of an inverse agonist of the peripheral cannabinoid receptor (CB(2)), 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.
authors.affiliation: Department of Chemistry, Xavier University of Louisiana, 1 Drexel Dr, New Orleans, LA 70125, USA.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
authors.forename: Peng
authors.initials: P
authors.lastname: Ma
authors.forename: Richard B
authors.initials: RB
authors.lastname: Cole
authors.forename: Guangdi
authors.initials: G
authors.lastname: Wang
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D007213:Indomethacin / Q000031:analogs & derivatives* / Q000378:metabolism; D008862:Microsomes, Liver / Q000378:metabolism*; D009025:Morpholines / Q000378:metabolism*; D051381:Rats; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors*; D013056:Spectrophotometry, Ultraviolet; D053719:Tandem Mass Spectrometry
chemical_list: D009025:Morpholines; D043885:Receptor, Cannabinoid, CB2; C471852:indomethacin morpholinylamide; D007213:Indomethacin