Nimodipine

Nimodipine is an inhibitor of L-type voltage-gated calcium (Ca_V) channels.¹ It is selective for Ca_V1.2 over Ca_V1.3 channels (IC₅₀s = 0.139 and 2.7 µM, respectively), as well as R-, N-, and P/Q-type Ca_v channels at 10 µM.^1,2 Nimodipine (0.72-24 nM) inhibits contractions induced by potassium, but not norepinephrine, in isolated rabbit aortic strips.³ It increases cerebral blood flow in anesthetized dogs when administered sublingually at doses ranging from 0.01 to 1 mg/kg. Nimodipine decreases necrosis of hippocampal CA1 pyramidal neurons and reduces increases in spontaneous movement and contralateral circling 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. Xu, W., and Lipscombe, D. Neuronal Ca_v1.3ɑ1 L-type channels activate at relatively hyperpolarized membrane potentials and are incompletely inhibited by dihydropyridines. J. Neurosci. 21(16), 5944-5951 (2001).

3. Kazda, S., and Towart, R. Nimodipine: A new calcium antagonistic drug with a preferential cerebrovascular action. Acta Neurochir. (Wien) 63(1-4), 259-265 (1982).

4. Babu, C.S., and Ramanathan, M. Post-ischemic administration of nimodipine following focal cerebral ischemic-reperfusion injury in rats alleviated excitotoxicity, neurobehavioural alterations and partially the bioenergetics. Int. J. Dev. Neurosci. 29(1), 93-105 (2011).