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

journal contribution
posted on 2023-11-02, 05:09 authored by RL BALSTER, FI CARROLL, JH GRAHAM, RS MANSBACH, Aziz RahmanAziz Rahman, A PHILIP, AH LEWIN, VM SHOWALTER
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 well 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.

History

Journal

DRUG AND ALCOHOL DEPENDENCE

Volume

29

Pagination

145-151

Location

Ireland

ISSN

0376-8716

eISSN

1879-0046

Language

English

Issue

2

Publisher

ELSEVIER SCI IRELAND LTD