Abstract

Structure-activity relationship studies on two mescaline analogues have been conducted, using rats trained on a CAR buzzer-shock schedule. 3∶4-dimethoxyphenylethylamine has been shown to depress the CAR with an apparent bimodal distribution of peak activities, in contrast to the biphasic inhibitory and excitatory effect of mescaline. The effect of this dimethoxy compound is similar to that previously reported for a protein fraction from schizophrenic plasma; this is of particular interest as six groups have recently reported the isolation of this compound from schizophrenic urine. The effect of N:N-dimethylation of mescaline is to abolish its inhibitory action on the CAR and to augment its excitant action. The significance of these findings is discussed.

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