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 (Ki values <2 nM) and high SERT selectivity (DAT/SERT >1500 and NET/SERT >1500).
Original language | English (US) |
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Pages (from-to) | 8356-8364 |
Number of pages | 9 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 18 |
Issue number | 23 |
DOIs | |
State | Published - Dec 1 2010 |
Keywords
- Depression
- Dopamine transporters
- Meperidine
- Norepinephrine transporters
- Normeperidine
- Serotonin transporter
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry