A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects

Abraham Nudelman, Irit Gil-Ad, Nava Shpaisman, Igor Terasenko, Hanna Ron, Kinneret Savitsky, Yona Geffen, Abraham Weizman, Ada Rephaeli

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)2858-2862
Number of pages5
JournalJournal of Medicinal Chemistry
Volume51
Issue number9
DOIs
StatePublished - 8 May 2008
Externally publishedYes

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