Abstract

Butaclamol, a new neuroleptic agent, and its (+)- enantiomer caused a pronounced dose-related elevation of rat striatal homovanillic acid concentration in vivo . In addition, each blocked the dopamine-induced increase in adenyl cyclase activity of homogenates of the olfactory tubercle, a limbic area in the brain. The (-)-enantiomer of butaclamol did not exhibit these activities indicating a stereochemical specificity for dopamine receptor-blockade activity. The (+)-enantiomer was 2–3 times more potent than butaclamol, exhibiting activities similar to those of fluphenazine. The present findings are consistent with the existence of relationships between changes in dopamine turnover in the striatum and the production of extrapyramidal side effects and between changes in adenyl cyclase activity of olfactory tubercle and antipsychotic activity.

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