Design, Sythesis and Pharmacological Studies of Benzothiazolin-2-one Analogues as a Novel Anxiolytic and Antipanic - like Agents

A series of derivatives of ketanserin, a prototype 5-HT[2A] antagonist, were synthesized and evaluated for their binding profiles. Compound 6 was the most active of all tested compounds, as it displayed 5-HT[1A], 5-HT[2A],,and D[2], 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 weight, orally and intraperitoneally, respectively. These activities were obtained without significant sedative, myo-relaxant side effects, or catalepsy. Compound 6 is currently undergoing further pharmacological and toxicological investigations