Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine

SA Lomenzo, S Izenwasser, RM Gerdes, JL Katz…

Index: Lomenzo, Stacey A.; Izenwasser, Sari; Gerdes, Robert M.; Katz, Jonathan L.; Kopajtic, Theresa; Trudell, Mark L. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 23 p. 3273 - 3276

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Citation Number: 10

Abstract

A series of meperidine analogues was synthesized and the binding affinities for the dopamine and serotonin transporters were determined. The substituents on the phenyl ring greatly influenced the potency and selectivity of these compounds for the transporter binding sites. In general, meperidine (3) and its analogues were more selective for serotonin transporter binding sites and the esters 9 were more potent than the corresponding nitriles ...