CI-996

CI-996 is a potent, selective, orally active angiotensin II (Ang II) type 1 (AT1) receptor antagonist. In rat liver membranes CI-996 displaces specifically bind [¹²⁵I]Ang II with an IC₅₀ of 0.8 nM. CI-996 has blood pressure-lowering activity^[1]. In Vitro:In isolated rabbit aorta CI-996 produces a concentration-dependent inhibition of Ang II-induced contraction and decreased the maximal contractile response to Ang II. CI-996 has no effect on the contractile responses to KCl, norepinephrine or endothelin^[1]. In Vivo:In anesthetized, ganglionic-blocked rats CI-996 produces dose-dependent inhibition of the Ang II pressor dose-response curve with an IC₅₀ of 6.2 μg/kg/min i.v^[1].
Orally administered CI-996 dose dependently loweres mean arterial blood pressure in conscious renal hypertensive rats, conscious sodium-depleted dogs, conscious sodium-depleted monkeys and conscious renal hypertensive monkeys^[1].