Nifedipine Inhibitor CAS No. 21829-25-4

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KI0880	Nifedipine	50 mg	$154

Chemical Characteristic

Product Name	Nifedipine
Synonyms	Adalat CC, Procardia
CAS No.	21829-25-4
Molecular Weight	346.33
Formula	C₁₇H₁₈N₂O₆
Chemical Structure

Biological activities

Nifedipine is a dihydropyridine calcium channel blocker. Nifedipine is used to treat the ianginal and hypertensive disease. The IC50 of nifedipine is 4.1 nM against Ca²⁺-induced contractions.^[1] Nifedipine inhibits atherogenesis but not reduces hypercholesterolemia.^[2] Nifedipine slows down the rate of transformation of smooth muscle cells from a contractile to a synthetic phenotype and inhibit initiation of DNA synthesis as well as cellular proliferation of arterial smooth muscle cells.^[3] Nifedipine significantly improves lysosomal and cytoplasmic cholesteryl ester (CE) hydrolase activity in normal SMC via increased levels of intracellular cyclic AMP.^[4] Nifedipine (0.003 to 3.0 µM) significantly dose-dependently reverses intrinsically existing tone in both tracheal spirals and parenchymal strips. Nifedipine also prevents the constriction of tracheal spirals and parenchymal strips induced by two different agonists, histamine and carbachol.^[5] Nifedipine (20-30 mg) given orally, effectively and rapidly reduces uterine activity, decreasing both amplitude and frequency of uterine contractions, and reduces basal tone in vivo.^[6]

References

[1] Burges RA, et al. Calcium channel blocking properties of amlodipine in vascular smooth muscle and cardiac muscle in vitro: evidence for voltage modulation of vascular dihydropyridine receptors. J Cardiovasc Pharmacol. 1987, 9(1): 110-119. 閵嗏偓閵嗏偓 [2] Watanabe N, et al. Nifedipine suppressed atherosclerosis in cholesterol-fed rabbits but not in Watanabe heritable hyperlipidemic rabbits. Artery. 1987, 14(5): 283-294. 閵嗏偓閵嗏偓 [3] Nilsson J, et al. The calcium antagonist nifedipine inhibits arterial smooth muscle cell proliferation. Atherosclerosis. 1985, 58(1-3): 109-122. [4] Etingin OR, et al. Nifedipine increases cholesteryl ester hydrolytic activity in lipid-laden rabbit arterial smooth muscle cells. A possible mechanism for its antiatherogenic effect. J Clin Invest. 1985, 75(5): 1554-1558. 閵嗏偓閵嗏偓 [5] Fanta CH, et al. Inhibition of bronchoconstriction in the guinea pig by a calcium channel blocker, nifedipine. Am Rev Respir Dis. 1982, 125(1): 61-66. 閵嗏偓閵嗏偓 [6] Ulmsten U, et al. Relaxing effects of nifedipine on the nonpregnant human uterus in vitro and in vivo. Obstet Gynecol. 1978, 52(4): 436-441. 閵嗏偓閵嗏偓

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