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KI0658Nimotop50 mg$154

Chemical Characteristic

Product NameNimotop
SynonymsNimodipine
CAS No.66085-59-4
Molecular Weight 418.44
FormulaC21H26N2O7
Chemical Structure

Biological activities

Nimotop is a dihydropyridine calcium channel blocker. The IC50 of nimotop is 14.9 nM against calcium channel. Nimotop possesses partition coefficients with a Kp of 187.[1] Nimotop inhibits contraction and rhythmic activity with an IC50 of 0.08 nM.[2] Nimotop blocks the internal calcium elevation in chronically depolarized rat cerebellar granule neurons with an IC50 of 0.45 nM.[3] In rats and baboons with middle cerebral artery occlusion, nimotop reduces neurological deficits without an increase in intracranial pressure or brain edema. Nimotop also improve memory in brain-damaged or old rats, restore sensorimotor function and abnormal walking patterns of old rats, and accelerate acquisition of associative learning in aging rabbits.[4] Nimotop dose-dependently decreases the DA metabolite 3-methoxytyramine (3-MT) in striatum and the limbic region. Nimotop markedly reduces the accumulation of 3-MT induced by pargyline. In addition, nimotop decreases concentrations of DA and homovanillic acid (HVA) in the limbic region but not in striatum.[5]

Protocols

Nimotop is dissolved in polyxoyethylated castor oil.[5]

References

[1] Yiu Sh, et al.Synthesis of valproate, valerate, and 1-methyl-1, 4-dihydropyridyl-3-carbonyloxy ester derivatives of Hantzsch 1,4-dihydropyridines as potential prodrugs and their evaluation as calcium channel antagonist and anticonvulsant agents. Drug Development Research, 1999, 48(1): 26-37.
[2] Godfraind T, et al. Calcium antagonists and vasoconstrictor effects in intracerebral microarterioles. Stroke. 1990, 21(12 Suppl): IV59-63. 閵嗏偓閵嗏偓
[3] Marchetti C, et al. High affinity block by nimodipine of the internal calcium elevation in chronically depolarized rat cerebellar granule neurons. Neurosci Lett. 1996, 207(2): 77-80. 閵嗏偓閵嗏偓
[4] Scriabine A, et al. Pharmacological basis for the use of nimodipine in central nervous system disorders. FASEB J. 1989, 3(7): 1799-1806. 閵嗏偓閵嗏偓
[5] Pileblad E, et al. In vivo effects of the Ca2+-antagonist nimodipine on dopamine metabolism in mouse brain. J Neural Transm. 1986, 66(3-4): 171-187. 閵嗏偓閵嗏偓

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