Clevidipine

Clevidipine is a selective, short-acting L-type calcium channel antagonist with an IC₅₀ of 7.1 nM. Clevidipine can competitively bind to calcium channels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury^[1]. In Vivo:Clevidipine (0.3 nmol/kg/min; coronary artery infusion; single; 15 minutes) reduces infarct size and protect coronary endothelial function in a porcine myocardial ischemia-reperfusion model, and its protective effect depends on the bioavailability of nitric oxide (NO)^[2].
Clevidipine (1.0 mg/kg; intravenous injection; single) shows rapid blood clearance in rats, mainly distributed in the heart and brain, and its metabolite H152/81 has a longer elimination half-life^[3].