Lemildipine is a new blocker of dihydropyridine calcium entry.

Lemildipine produces a significant decrease in the blood pressure of spontaneously hypertensive rats (SHR). Lemildipine is 1.4 times stronger than Nifedipine; the ED30 values of Lemildipine and Nifedipine are 10.2 mg/kg and 14.3 mg/kg, respectively[2]. Gerbils are treated intraperitoneally with Lemildipine (0.1-3 mg/kg) just after release of the occlusion. Four days after the ischemia, they are fixed by perfusing 10% buffered-formalin, and the neuronal cell density (NCD, cell/mm) in the CA1 subfield is estimated under microscopy. The average NCD in the ischemic control group is 43±10.8 cells/mm, whereas Lemildipine (3 mg/kg) significantly ameliorates DND with an average NCD of 143±24.2 cells/mm (P<0.01). Lemildipine (3-30 mg/kg; p.o.), in normal Wistar rats (NWR), produces a mild lowering of blood pressure. Lemildipine(p.o.; 3, 10, 30 mg/kg) produces a significant decrease in systolic blood pressure dose-dependently. Lemildipine (3 mg/kg) significantly inhibits delayed neuronal death (DND) at 1, 2 and 4 weeks after transient ischemia: the average NCD of the Lemildipine and ischemic control groups are 80±9.4 (P<0.01) and 43±7.7 cells/mm, 92±13.7 (P<0.05) and 52±9.3 cells/mm, and 57±5.0 (P<0.01) and 43±12.4 cells/mm, respectively. Lemildipine shows a protective effect on DND in the hippocampal CA1 subfield after transient forebrain ischemia, in this experiment, and its effect persisted for up to 4 weeks[1]. The maximum decrease is observed 1-3 hr after administration. Comparing the hypotensive potency of Lemildipine and Nifedipine, their dose-response curves at the maximum response during the observation (for 24 hr) are analyzed by the least squares method, and the dose of 30% decrease in blood pressure from the control level (ED30) are used as a measure of their potency.