Further evidence for a dopamine reuptake pharmacophore. The effect of N-methylation on threo-methylphenidate and its analogs

被引：25

作者：

Froimowitz, M

Deutsch, HM

Shi, Q

Wu, KM

Glaser, R

Adin, I

George, C

Schweri, MM

机构：

[1] GEORGIA INST TECHNOL,SCH CHEM & BIOCHEM,ATLANTA,GA 30332

[2] BEN GURION UNIV NEGEV,DEPT CHEM,IL-84105 BEER SHEVA,ISRAEL

[3] USN,RES LAB,STRUCT MATTER LAB,WASHINGTON,DC 20375

[4] MERCER UNIV,SCH MED,DIV BASIC MED SCI,MACON,GA 31207

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(97)00193-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-methyl derivatives of methylphenidate and four analogs were synthesized and assayed for affinity at the dopamine transporter. The binding affinities of the N-methyl compounds were consistently lower by a factor ranging from 4 to 30 as compared with the corresponding secondary amine. This is consistent with the predictions of a pharmacophore model of compounds that bind to the dopamine transporter. (C) 1997 Elsevier Science Ltd.

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页码：1213 / 1218

页数：6

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