PRENYLAMINE DERIVATIVES AS BLOCKERS OF THE VESICULAR TRANSPORTER FOR DOPAMINE - A QUANTITATIVE STRUCTURE-ACTIVITY STUDY

Authors
VACCARI A SABA PL CALDIROLA MP BIJLOO GJ TIMMERMAN H
Citation
A. Vaccari et al., PRENYLAMINE DERIVATIVES AS BLOCKERS OF THE VESICULAR TRANSPORTER FOR DOPAMINE - A QUANTITATIVE STRUCTURE-ACTIVITY STUDY, European journal of medicinal chemistry, 32(1), 1997, pp. 53-57
Citations number
20
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
32
Issue
1
Year of publication
1997
Pages
53 - 57
Database
ISI
SICI code
0223-5234(1997)32:1<53:PDABOT>2.0.ZU;2-S
Abstract
A new series of diphenylalkylamine congeners of prenylamine have been assayed in binding experiments on rat striatal membrane preparations. The aim was to ascertain the influence of structural modifications and lipophilicity on their interaction with the [H-3]tyramine-labelled ve sicular transporter for dopamine. Thirteen compounds potently inhibite d the specific binding of [H-3]tyramine, with nanomolar K-i values in the range of those of established markers for the vesicular transporte r of dopamine. Less lipophilic compounds displayed higher affinity for the energy-dependent amine transporter.