Kimia Biosciences Limited

Azelnidipine

General Information:

Azelnidipine is a dihydropyridine calcium channel blocker. it has a gradual onset and has a long-lasting hypotensive effect, with minimal increase in heart rate [L1379]. It is currently being studied for post-ischemic stroke management [L1380]. Azelnidipine is a vasodilator that induces a gradual decrease in blood pressure in hypertensive patients. Unlike other members of its drug class, azelnidipine does not induce reflex tachycardia due to vasodilation. This is likely due to the fact that it elicits a gradual fall in blood pressure. It also exhibits a prolonged hypotensive effect and has been shown to have a strong anti-arteriosclerotic action in vessels due to its high affinity for vascular tissue and antioxidative activity.

CAS No.

123524-52-7

Therapeutic Category:

Anti-Hypertensive drugs

IUPAC Name:

3-(1-Benzhydrylazetidin-3-yl) 5-isopropyl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

Molecular Formula:

C33H34N4O6

Molecular Weight:

C33H34N4O6

Molecular Structure:

Azelnidipine

Mechanism of Action

Azelnidipine inhibits trans-membrane Ca2+ influx through the voltage-dependent channels of smooth muscles in vascular walls. Ca2+ channels are classified into various categories, including L-type, T-type, N-type, P/Q-type, and R-type Ca2+ channels. The L-type Ca2+ channels. Normally, calcium induces smooth muscle contraction, contributing to hypertension. When calcium channels are blocked, the vascular smooth muscle does not contract, resulting in relaxation of vascular smooth muscle walls and decreased blood pressure.