STRUCTURE-ACTIVITY STUDIES ON AMPHETAMINE ANALOGS USING DRUG DISCRIMINATION METHODOLOGY
STRUCTURE-ACTIVITY STUDIES ON AMPHETAMINE ANALOGS USING DRUG DISCRIMINATION METHODOLOGY
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DOI：
10.1016/s0091-3057(84)80071-4
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发表时间：
1984-01-01
影响因子：
3.6
通讯作者：
MCKENNEY, JD
中科院分区：
文献类型：
--
作者：
GLENNON, RA;YOUNG, R;MCKENNEY, JD
Animals (rats) trained to discriminate 1.0 mg/kg of S(+)-amphetamine sulfate from saline, using a standard operant training procedure, were administered doses of various amphetamine analogs in tests of stimulus generalization to study structure-activity relationships (SAR). The types of structural variation of the amphetamine molecule that were investigated included benz-fusion of the aromatic nucleus, .alpha.-demethylation of the alkyl side chain, conversion of the benzylic methylene to a carbonyl group and conformational restriction of the side chain. Benz-fusion and .alpha.-demethylation appear to have a detrimental effect on activity in that none of these analogs produced amphetamine-appropriate responding. The carbonylated analog, i.e., cathinone, was equipotant with amphetamine. As with amphetamine, the S-isomer of cathinone was more active than its enantiomer. With respect to the conformationally-restricted analogs, the most potent compound was 2-aminotetralin which was about half as active as racemic amphetamine.
