NEW, POTENT COCAINE ANALOGS - LIGAND-BINDING AND TRANSPORT STUDIES IN RAT STRIATUM

被引：89

作者：

BOJA, JW

CARROLL, FI

RAHMAN, MA

PHILIP, A

LEWIN, AH

KUHAR, MJ

机构：

[1] NIDA,ADDICT RES CTR,NEUROSCI BRANCH,POB 5180,BALTIMORE,MD 21224

[2] RES TRIANGLE INST,RES TRIANGLE PK,NC 27709

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1990年 / 184卷 / 2-3期

关键词：

Cocaine binding sites; Dopamine transporters; Dopamine uptake; Striatum;

D O I：

10.1016/0014-2999(90)90627-I

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Two potent cocaine analogs have been developed that have the highest known affinities for the cocaine binding site in rat striatum. Both 3β-(4-chlorophenyl)- (RTI-COC-31) and 3β-(4-methylphenyl)-tropane-2-carboxylic acid methyl ester (RTI-COC-32) compete for [3H]WIN 35,428 and [3H]mazindol binding with a IC50 that is 100 times more potent than that of (-) cocaine. Additionally, these compounds inhibit [3H]dopamine uptake with a similar, high potency. These results may lead to the development of high affinity probes for the cocaine binding site. © 1990.

引用

页码：329 / 332

页数：4

共 9 条

[1]

BERGMAN J, 1989, J PHARMACOL EXP THER, V251, P150

[2] [H-3] COCAINE BINDING AND INHIBITION OF [H-3] DOPAMINE UPTAKE IS SIMILAR IN BOTH THE RAT STRIATUM AND NUCLEUS ACCUMBENS [J].