Zoniporide hydrochloride is a selective inhibitor of NHE-1 with IC50 of 14 nM which is >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride shows an IC50 of 59 nM for NHE-1-dependent swelling of human platelets.

In rats, Zoniporide hydrochloride (1 mg/kg; i.v.) shows the AUC0-∞ and t1/2 are 0.07 μg h/mL and 0.5 hours, respectively[1]. In open chest anesthetized rabbits, Zoniporide hydrochloride (0.25, 1, 4 mg/kg; i.v.) dose-dependently reduces infarct size with an ED50 of 0.45 mg/kg/h. Zoniporide hydrochloride exhibits moderate plasma protein binding with t1/2 of 1.5h in monkeys[2].