Bibliographic Information

Design, synthesis and pharmacological studies of benzothiazolin-2-one analogues as a novel anxiolytic and antipanic-like agents.     Diouf, Ousmane; Poupaert, Jacques H.; Salim, Maher; Lesieur, Daniel; Isa, Majed.    Institut de Chimic Pharmaceutique,  Lillc,  Fr.    Saudi Pharmaceutical Journal  (2000),  8(2-3),  91-100.  CODEN: SPJOEM  ISSN: 1319-0164.  Journal  written in English.    CAN 135:137    AN 2000:820871    CAPLUS  

Abstract

A series of derivs. of ketanserin, a prototype 5-HT2A antagonist, were synthesized and evaluated for their binding 5-HT receptor profiles.  The ketanserin deriv. S-21357-1 was the most active of all tested compds., as it displayed 5-HT1A, 5-HT2A and D2 binding affinities at nanogram levels.  It was found to exhibit anxiolytic and antipanic-like effects in mice, in doses of 0.25 mg and 0.125 mg/kg body wt., orally and i.p., resp.  These activities were obtained without significant sedative, myorelaxant side effects, or catalepsy.  S-21357-1 is currently undergoing further pharmacol. and toxicol. investigations.  

Indexing -- Section 1-3  (Pharmacology)