Nilvadipine-d4

Nilvadipine-d₄ is intended for use as an internal standard for the quantification of nilvadipine by GC- or LC-MS. 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

1.Furukawa, T., Yamakawa, T., Midera, T., et al.Selectivities of dihydropyridine derivatives in blocking Ca2+ channel subtypes expressed in Xenopus oocytesJ. 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 ratsTohoku 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 barrierMol. 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 ratsExp. Brain Res.83(2)434-438(1991)