Description
Manidipine is a dihydropyridine L- and T-type calcium channel blocker. It blocks recombinant rabbit L-type (α
1Cα
2/δβ
1a) and human T-type (α
1H) calcium channels expressed in
Xenopus oocytes and native L-type channels in dissociated guinea pig cardiac ventricular cells (IC
50 = 2.6 nM). Manidipine inhibits intracellular calcium increases induced by endothelin-1 (ET-1; ) in A
7r
5 rat vascular smooth muscle cells (ED
50 = 1 nM) and potassium-induced contraction of isolated dog femoral and portal veins (IC
50s = 24 and 2.1 nM, respectively).
In vivo, it lowers blood pressure in spontaneously hypertensive rats (SHRs) when administered at a dose of 10 mg/kg and inhibits left ventricular hypertrophy in rats induced by isoproterenol when administered at a dose of 3 mg/kg. Formulations containing manidipine have been used in the treatment of hypertension.
Uses
Manidipine (Manyper) is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. It
