Manidipine is a dihydropyridine L- and T-type calcium channel blocker.
1,2,3 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; Item No.
24127) 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).
4,5 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 (Item No.
15592) when administered at a dose of 3 mg/kg.
6,7 Formulations containing manidipine have been used in the treatment of hypertension.
