Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 9, Pages 2858-2862Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm7012453
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The perphenazine and fluphenazine GABA esters 3 and 4 evaluated in rat models for antipsychotic activity displayed a significant decrease of catalepsy associated with increased prolactin blood levels. Efficacy was evaluated in the D-amphetamine-induced hyperactivity model, where perphenazine abolished hyperactivity and induced sedation and catalepsy, whereas 3 reduced hyperactivity without sedation or catalepsy. Thus, 3 (BL-1020) constitutes a prototype of novel antipsychotics possessing GABAergic activity. A phase II study is in progress.
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