Journal of Medicinal Chemistry p. 1079 - 1082 (1991)
Update date:2022-07-31
Topics:
Cannon, Joseph G.
Qijie, Pang
The isomeric monomethyl ether derivatives of (RS)-9,10-dihydroxyaporphine ("isoapomorphine") were synthesized unequivocally as possible metabolites in catechol-O-methyltransferase (COMT) mediated O-methylation reactions.In vitro incubation studies revealed that isoapomorphine is not a substrate for the COMT using experimental conditions under which apomorphine (10,11-dihydroxyaporphine) is converted in high yield into its 10-methyl ether, apocodeine.The in vivo dopaminergic inactivity of isoapomorphine (as compared with that of apomorphine) seems to be due to factors other than metabolic inactivation by COMT.
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