Captopril disulfide

Captopril disulfide (SQ 14551) is an orally active disulfide dimer prodrug. Captopril disulfide is metabolized to Captopril and acts as a Bradykinin potentiator. Captopril disulfide enhances the vasodilatory effect of Bradykinin in anesthetized rats and the contractile response of isolated guinea pig ileum to Bradykinin. Captopril disulfide exhibits antihypertensive activity in spontaneously hypertensive rats. Captopril disulfide can be used in hypertension-related research^[1][2]. In Vitro:Captopril disulfide (0.1-10 μM) potentiates 0.01 μM bradykinin-induced contractions in isolated guinea pig ileum, with no significant activity at 0.1 μM and 1.0 μM, a 285% of control potentiation at 10 μM, and an EC₅₀ of 3.0 μM^[2]. In Vivo:Following single administration of Captopril disulfide (10 mg/kg; p.o., i.v.) to Sprague-Dawley rats, the active captopril monomer is rapidly generated, producing significant plasma ACE inhibitory effects, and captopril-related substances accumulate in the kidneys, liver, and lungs^[1].
Captopril disulfide (0.1-1.0 mg/kg; i.v.; single bolus) enhances bradykinin-induced vasodilation in anesthetized rats^[2].
Captopril disulfide (10 mg/kg; p.o.; single administration) exerts a significant hypotensive effect in spontaneously hypertensive rats^[2].