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