Early clinical experience with flesinoxan, a new selective 5-HT_1A receptor agonist

Abstract

Flesinoxan hydrochloride has been shown in pharmacological experiments to be a potent and selective 5-HT_1A receptor agonist with centrally-mediated antihypertensive properties. Flesinoxan lowers blood pressure in various species, and the effect lasts for more than four hours after a single administration [1]. The cardiovascular profile of the compound includes a reduction of total peripheral resistance, a small, vagally mediated decrease in heart rate, little or no effect on cardiac output, no direct negative inotropic effect and strong renal vasodilatation. Further, no orthostatic hypotension or tachyphylaxis has been found [1, 2]. In the investigation reported here flesinoxan has been studied in normotensive and hypertensive human subjects. Special attention was paid to cardiovascular parameters, safety, tolerability, psychometric performance and pharmacokinetics of the drug after single and repeated doses.