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)