Literature DB >> 20980153

Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.

Xiaobo Gu1, Sari Izenwasser, Dean Wade, Amy Housman, Gerard Gulasey, Jill B Rhoden, Christopher D Savoie, David L Mobley, Stacey A Lomenzo, Mark L Trudell.   

Abstract

A series of benzyl esters of meperidine and normeperidine were synthesized and evaluated for binding affinity at serotonin, dopamine and norepinephrine transporters. The 4-methoxybenzyl ester 8b and 4-nitrobenzyl ester 8c in the meperidine series and 4-methoxybenzyl ester 14a in the normeperidine series exhibited low nanomolar binding affinities at the SERT (K(i) values <2nM) and high SERT selectivity (DAT/SERT >1500 and NET/SERT >1500).
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20980153      PMCID： PMC3713777          DOI： 10.1016/j.bmc.2010.09.060

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  27 in total

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