Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist.Target: α1-adrenoceptor; 5-HT1A receptorUrapidil hydrochloride is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system [1]. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system. Several studies have suggested that oral urapidil is effective and well tolerated when used as second-line therapy in patients with BP inadequately controlled with other agents. Urapidil has also been shown to improve glucose and lipid metabolism in hypertensive patients with concomitant diabetes and/or hyperlipidemia [2].
References:
[1]. Gross, G., G. Hanft, and N. Kolassa, Urapidil and some analogues with hypotensive properties show high affinities for 5-hydroxytryptamine (5-HT) binding sites of the 5-HT1A subtype and for alpha 1-adrenoceptor binding sites. Naunyn Schmiedebergs Arch Pharmacol, 1987. 336(6): p. 597-601.
[2]. Buch, J., Urapidil, a dual-acting antihypertensive agent: Current usage considerations. Adv Ther, 2010. 27(7): p. 426-43.