FURTHER EVIDENCE FOR A DOPAMINE REUPTAKE PHARMACOPHORE - THE EFFECT OF N-METHYLATION ON THREO-METHYLPHENIDATE AND ITS ANALOGS

Authors
FROIMOWITZ M DEUTSCH HM SHI Q WU KM GLASER R ADIN I GEORGE C SCHWERI MM
Citation
M. Froimowitz et al., FURTHER EVIDENCE FOR A DOPAMINE REUPTAKE PHARMACOPHORE - THE EFFECT OF N-METHYLATION ON THREO-METHYLPHENIDATE AND ITS ANALOGS, Bioorganic & medicinal chemistry letters, 7(9), 1997, pp. 1213-1218
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
9
Year of publication
1997
Pages
1213 - 1218
Database
ISI
SICI code
0960-894X(1997)7:9<1213:FEFADR>2.0.ZU;2-7
Abstract
N-methyl derivatives of methylphenidate and four analogs were synthesi zed and assayed for affinity at the dopamine transporter. The binding affinities of the N-methyl compounds were consistently lower by a fact or ranging from 4 to 30 as compared with the corresponding secondary a mine. This is consistent with the predictions of a pharmacophore model of compounds that bind to the dopamine transporter. (C) 1997 Elsevier Science Ltd.