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

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

文献索引: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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被引用次数: 10

摘要

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 ...