Synthesis and biological evaluation of meperidine analogues at monoamine transporters

SA Lomenzo, JB Rhoden, S Izenwasser…

Index: Lomenzo, Stacey A.; Rhoden, Jill B.; Izenwasser, Sari; Wade, Dean; Kopajtic, Theresa; Katz, Jonathan L.; Trudell, Mark L. Journal of Medicinal Chemistry, 2005 , vol. 48, # 5 p. 1336 - 1343

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Citation Number: 17

Abstract

A series of aryl-substituted meperidine analogues was synthesized, and the binding affinities were determined at the DAT, SERT, and NET as well as at μ-opioid receptors. Generally the analogues exhibited increased affinity for the DAT and SERT relative to meperidine but exhibited low binding affinity for the NET. The 2-naphthyl derivative 7f was the most potent ligand at the SERT (K i= 0.0072 μM) and was the most selective ligand for ...