Bibliographic Information

Novel Benzothiazolin-2-one and Benzoxazin-3-one Arylpiperazine Derivatives with Mixed 5HT1A/D2 Affinity as Potential Atypical Antipsychotics.     Taverne, Thierry; Diouf, Ousmane; Depreux, Patrick; Poupaert, Jacques H.; Lesieur, Daniel; Guardiola-Lemaitre, Beatrice; Renard, Pierre; Rettori, Marie-Claire; Caignard, Daniel-Henri; Pfeiffer, Bruno.    Institut de Chimie Pharmaceutique,  Lille,  Fr.    Journal of Medicinal Chemistry  (1998),  41(12),  2010-2018.  CODEN: JMCMAR  ISSN: 0022-2623.  Journal  written in English.    CAN 128:317202    AN 1998:298847    CAPLUS  

Abstract

Since 5HT properties (5HT1A agonism or 5HT2A antagonism) combined with D2 antagonism may lead to atypical antipsychotic drugs, 19 benzothiazolin-2-one and benzoxazin-3-one derivs. possessing the arylpiperazine moiety were prepd., and their binding profiles were studied.  All tested compds. displayed very high affinities for the 5HT1A and D2 receptors.  Therefore, further pharmacol. studies were carried out on selected compds.  This evaluation in rats clearly revealed potent antipsychotic properties along with a decrease of extrapyramidal side effects.  These derivs. are currently under preclin. development.  

Indexing -- Section 1-11  (Pharmacology)  
Section cross-reference(s): 28