

Supplier:
Alomone Labs Ltd.Cat no: N-150
Nimodipine
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 alpha1 subunit. The subunits CaV1.1-1-4 (alpha1S, alpha1C, alpha1D and alpha1F) form L-type Ca2+ channels and bind dihydropyridines (DHPs) with high affinity. Nimodipine is a strongly selective L-type Ca2+ channel blocker, with IC50 of 139 nM for Cav1.2 channel currents in Xenopus oocytes. At 1 μmпїЅNimodipine inhibits 90% of the Cav1.2 channel current at voltages between -20 and +40 mV.
Ca2+ antagonists block Ca2+ entry into cells, resulting in relaxation of smooth muscle and limitation of the cytotoxic effects of ischaemia in various organ systems. They are most frequently used for clinical conditions requiring vasodilatation, i.e hypertension and Raynaud's phenomenon. Other uses include treatment of supraventricular arrhythmias and angina. Nimodipine has been approved for treating vasospasm after subarachnoid haemorrhage.
Cytosolic free Ca2+ increases with aging and since this increase may be mediated by the voltage operated L-type Ca2+ channel on the neuronal cell body, chronic treatment with an L-channel blocker, like Nimodipine, might palliate the progression of and possibly prevent the majority of cases of AlzheimerпїЅs disease (AD).
A migraine attack is initiated by a cellular hypoxia that can cause an increase in the flow of calcium into the intracellular space, resulting in calcium overload and cellular dysfunction.
Nimodipine exhibits selective effects on cerebral vessels and seems to offer protection against the cerebral ischemia and hypoxia presumed to be operative during migraine attacks and indeed, the frequency and duration of migraine attacks are decreased by at least half in 69% of patients treated with this agent.
Ion Channel Modulators; Voltage - Gated Ca2+ Channel Blockers
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SPECIFICATIONS
Catalog Number
N-150
Size
1 gr
Purity
>99%
Concentration
0.1-100 uM
Shipping Temp
Room Temperature
Molecular Weight
418.4 da
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