Description
Benidipine hydrochloride is a new, long acting dihydropyridine calcium antagonist useful in the treatment of hypertension and angina pectoris. In experimental animals,
benidipine hydrochloride dose dependently induced hypotension with a potency of
6 and 12 times more than nifedipine and nicardipine, respectively. It also exhibited a
slow onset of action.
Description
Benidipine is an orally bioavailable blocker of L-, T-, and N-type calcium channels. In guinea pig ventricular cells benidipine has an IC
50 of 2.7 nM for calcium currents, determined using whole cell voltage clamp electrophysiology. It prevents oxidative stress dose-dependently
in vitro, decreases blood pressure in spontaneously hypertensive rats (at 3 and 10 mg/kg), and is neuroprotective for neural stem cells after oxidative stress-induced injury. Benidipine is also a competitive antagonist at mineralocorticoid receptors.
Chemical Properties
Yellow Crystalline Powder
Originator
Kyowa Hakko (Japan)
Uses
A dihydropyridine calcium channel blocker. Antihypertensive.
Biological Activity
Orally active antihypertensive agent which displays a wide range of activities in vitro and in vivo . Inhibits L-, N- and T-type Ca 2+ channels. Also inhibits aldosterone-induced mineralocorticoid receptor activation. Exhibits cardioprotective and antiartherosclerotic effects.
Safety Profile
A poison by ingestion,intraperitoneal, and intravenous routes. When heated todecomposition it emits toxic vapors of NOx and HCl.
storage
room temperature (desiccate)
