POTENT SUBSTITUTED-3-BETA-PHENYLTROPANE ANALOGS OF COCAINE HAVE COCAINE-LIKE DISCRIMINATIVE STIMULUS EFFECTS

被引：20

作者：

BALSTER, RL ^{[1
]}

CARROLL, FI ^{[1
]}

GRAHAM, JH ^{[1
]}

MANSBACH, RS ^{[1
]}

RAHMAN, MA ^{[1
]}

PHILIP, A ^{[1
]}

LEWIN, AH ^{[1
]}

SHOWALTER, VM ^{[1
]}

机构：

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

来源：

DRUG AND ALCOHOL DEPENDENCE | 1991年 / 29卷 / 02期

关键词：

COCAINE; ANALOGS; DRUG DISCRIMINATION; DOPAMINE UPTAKE; RATS;

D O I：

10.1016/0376-8716(91)90043-X

中图分类号：

R194 [卫生标准、卫生检查、医药管理];

学科分类号：

摘要：

Two novel phenyltropane analogs of cocaine, 3-beta-(4-chlorophenyl) tropane-2-beta-carboxylic acid methyl ester (RTI-COC-31) and 3-beta-(4-methylphenyl) tropane-2-beta-carboxylic acid methyl ester (RTI-COC-32), were evaluated for cocaine-like discriminative stimulus effects in rats. Two groups of rats were trained to discriminate 10 mg/kg cocaine from saline using a standard 2-lever discrimination procedure with correct-lever responding reinforced under a fixed-ratio 20 schedule of food reinforcement. One group of rats was used to evaluate RTI-COC-31 and the unsubstituted-3-beta-phenyltropane reference compound WIN 35,065-2 in substitution tests. Another group of rats was used to evaluate RTI-COC-32. For purposes of comparison, a cocaine dose-effect curve was also determined in each group. Both RTI-COC-31 and RTI-COC-32, as weil as WIN 35,065-2, substituted completely for cocaine. RTI-COC-31 was 26.8-fold and RTI-COC-32 was 6-fold more potent than cocaine for producing cocaine-lever responding. The potent cocaine-like effects of the RTI analogs in vivo correspond with their high affinities for a cocaine recognition site on the dopamine transporter, providing further evidence that this site may mediate behavioral effects of cocaine relevant to its abuse.

引用

页码：145 / 151

页数：7

共 21 条

[1]

Balster RL, 1990, COMP PERCEPTION, P127

[2]

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

[3] NEW, POTENT COCAINE ANALOGS - LIGAND-BINDING AND TRANSPORT STUDIES IN RAT STRIATUM [J].