Forasartan (SC-52458) is a potent, specific, competitive and reversible angiotensin II receptor (AT1 receptor) antagonist with binding Ki value of 2.9 nM.
Forasartan (SC-52458) is a potent inhibitor of [125I]AII binding to AT1 receptors in rat adrenal cortex and uterine smooth muscle membranes (IC50 values of 2.8 and 6.9 nM, respectively).
Forasartan (SC-52458) shows no effect on the activity of angiotensin converting enzyme (ACE) or renin in vitro.
Forasartan administration selectively inhibits L-type calcium channels in the plateau component of the smooth muscle cells, favoring relaxation of the smooth muscle.
Forasartan also decreases heart rate by inhibiting the positive chronotropic effect of high frequency preganglionic stimuli.
In dogs, it was found to block the pressor response of Angiotensin II with maximal inhibition, 91%.
Daily treatment with Forasartan (SC-52458) at 20, 30, and 50 mg/kg by gavage for 4 days decreased blood pressure (BP) in conscious, spontaneously hypertensive rats (SHR).