SYNTHESIS AND LIGAND-BINDING OF COCAINE ISOMERS AT THE COCAINE RECEPTOR

被引：78

作者：

CARROLL, FI ^{[1
]}

LEWIN, AH ^{[1
]}

ABRAHAM, P ^{[1
]}

PARHAM, K ^{[1
]}

BOJA, JW ^{[1
]}

KUHAR, MJ ^{[1
]}

机构：

[1] NIDA,ADDICT RES CTR,NEUROSCI BRANCH,BALTIMORE,MD 21224

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 03期

关键词：

D O I：

10.1021/jm00107a003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cocaine binding site at the dopamine transporter has been found to be stereoselective. Thus, the seven possible stereoisomers of (-)-cocaine have been synthesized and found to inhibit [H-3]-2-beta-carbomethoxy-3-beta-(4-fluorophenyl)tropane ([H-3]WIN 35,428) with potencies ranging from 1/60 to 1/600 of that of (-)-cocaine. The synthesis and characterization of all new compounds is presented.

引用

页码：883 / 886

页数：4

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