Background:

Tasosartan is a long-acting angiotensin II (AngII) receptor antagonist.

Tasosartan is an orally active nonpeptide AngII antagonist that has demonstrates specific and selective AT1 receptor antagonistic activity in vitro. IC50 for inhibition of specific binding of 125I-AngII to rat adrenal membrane in the absence of proteins in binding buffer is 1.2±0.6 nM[1].

Administration of Tasosartan at doses of 1.0 and 3.0 mg/kg (iv) significantly (p<0.05) attenuates the pressor response to angiotensin-II in rats[2].

[1]. Maillard MP, et al. Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54. [2]. Elokdah HM, et al. Novel human metabolites of the angiotensin-II antagonist Tasosartan and their pharmacological effects. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1967-71.