THE EFFECTS OF ALKYL SUBSTITUENTS AT THE 6-POSITION OF COCAINE ANALOGS ON DOPAMINE TRANSPORTER BINDING-AFFINITY AND DOPAMINE UPTAKE INHIBITION

Citation
Sa. Lomenzo et al., THE EFFECTS OF ALKYL SUBSTITUENTS AT THE 6-POSITION OF COCAINE ANALOGS ON DOPAMINE TRANSPORTER BINDING-AFFINITY AND DOPAMINE UPTAKE INHIBITION, Medicinal chemistry research, 8(1-2), 1998, pp. 35-42
Citations number
33
Categorie Soggetti
Chemistry Medicinal
ISSN journal
10542523
Volume
8
Issue
1-2
Year of publication
1998
Pages
35 - 42
Database
ISI
SICI code
1054-2523(1998)8:1-2<35:TEOASA>2.0.ZU;2-T
Abstract
A series of 6-alkyl-3 beta-benzyl-2-(methoxycarbonylmethyl)tropane ana logues were synthesized and evaluated as cocaine binding-site ligands at the dopamine transporter (DAT). The in vitro inhibition of [3H]dopa mine and the DAT binding affinity (K-i, [H-3]WIN 35,428) were measured in rat caudate putamen tissue. Generally, substitution at the B-posit ion was found to reduce ligand potency.