Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands |
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| Authors: | Gu Xiaobo Izenwasser Sari Wade Dean Housman Amy Gulasey Gerard Rhoden Jill B Savoie Christopher D Mobley David L Lomenzo Stacey A Trudell Mark L |
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| Affiliation: | Department of Chemistry, University of New Orleans, LA 70148, USA. |
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| 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). |
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