Nilvadipine

Nilvadipine is a dihydropyridine L-type calcium channel blocker.¹ It is selective for L-type over N-, P/Q-, and R-type calcium channels at 10 μM. Nilvadipine (10 mg/kg per day, p.o.) inhibits increases in systolic blood pressure induced by chronic intravenous infusion of the peptide vasoconstrictor endothelin in rats.² It decreases cortical and hippocampal amyloid-β burden in the APPsw (Tg2576) and PS1/APPsw transgenic mouse models of Alzheimer's disease when administered at a dose of 0.03% (w/w) in the diet for 17 and 10 months, respectively.³ Nilvadipine (3.2 mg/kg, s.c.) reduces infarct volume in a rat model of focal cerebral ischemia induced by middle cerebral artery occlusion (MCAO).⁴

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1. Furukawa, T., Yamakawa, T., Midera, T., et al. Selectivities of dihydropyridine derivatives in blocking Ca²⁺ channel subtypes expressed in Xenopus oocytes. J. Pharmacol. Exp. Ther. 291(2), 464-473 (1999).

2. Yasujima, M., Abe, K., Kanazawa, M., et al. Antihypertensive effect of captopril and enalapril in endothelin-infused rats. Tohoku J. Exp. Med. 163(3), 219-227 (1991).

3. Paris, D., Bachmeier, C., Patel, N., et al. Selective antihypertensive dihydropyridines lower Aβ accumulation by targeting both the production and the clearance of Aβ across the blood-brain barrier. Mol. Med. 17(3-4), 149-162 (2011).

4. Kawamura, S., Yasui, N., Shirasawa, M., et al. Effects of a Ca²⁺ entry blocker (nilvadipine) on acute focal cerebral ischemia in rats. Exp. Brain Res. 83(2), 434-438 (1991).