Manidipine dihydrochloride (Manidipine 2HCl) is a potent calcium channel blocker for Ca2+ current(IC50=2.6 nM).

Ca2+ channel:2.6 nM

At nanomolar concentrations, Manidipine effectively modulates gene transcription involved in the inflammatory transformation of mesangial cells. Manidipine inhibits the coronary artery (pIC50=9.3 nM) and renal artery (pIC50=9.1 nM). Additionally, Manidipine decreases Ca2+ flux at concentrations above 0.1 nM and blocks Ca2+ flux at 100 nM.

In hypertensive rats, oral administration of Manidipine (3 mg/kg and 10 mg/kg) reduced systolic blood pressure in a dose-dependent manner. When administered at a dose of 10 mg/kg, Manidipine was able to normalize blood pressure within 1 to 3 hours post-administration.

The mitogenic effect is measured by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, 1 × 105 quiescent cells is seeded into a 25-mL cell culture bottle and kept in low serum medium (0.1% FCS). On the following day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. The medium is replaced each day, and the cells are counted at days 1, 3 and 5.(Only for Reference)