Nifedipine was initially developed for the prophylaxis of angina symptoms, and then later used as an anti-hypertensive agent. Nifedipine acts by inhibiting the transmembrane influx of calcium into cardiac and vascular smooth muscle cells, thus reducing muscle contraction and has predominantly vasodilatory effects on arteries with minimal effects on the myocardium and cardiac conduction. For the same reason Nifedipine is also useful in the reduction of the frequency and severity of the attacks in Raynaud’s phenomenon, an episodic vasospasm of the peripheral arteries.
产品描述
A Blocker of L-type CaV Channels
产品形式
Native voltage-gated Ca2+ channels (VGCC, CaV) are pharmacologically classified into at least five different subclasses (L-, N-, P-, Q-, and R-type), the characteristics of which are determined by the pore- forming a1 subunit. The subunits CaV1.1-1.4 (α1S, α1C, α1D and α1F) form L-type Ca2+ channels and bind dihydropyridines (DHPs) with high affinity. Nifedipine, a DHP, is a selective L-type Ca2+ channel blocker3. 10 µM Nifedipine inhibits ~65% of the L-type channel current at a holding potential of -80 mV, in Xenopus oocytes.