Cat. No. Name Size Price Add Cart
KI0674Felodipine10 mg$155.2
Felodipine50 mg$496

Chemical Characteristic

Product NameFelodipine
SynonymsPlendil, Renedil
CAS No.72509-76-3
Molecular Weight 384.25
FormulaC18H19Cl2NO4
Chemical Name4-(2,3-dichlorophenyl)-1,4-dihyro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl ester
SmilesC1(=C(C(C(=C(N1)C)C(=O)OCC)c1c(c(ccc1)Cl)Cl)C(=O)OC)C
Chemical Structure

Biological activities

Felodipine is a calcium channel blocker. The IC50 value of felodipine is 3 nM against isometric force development in K+-depolarized aortic smooth muscle strips.[1] Felodipine is 100-fold more potent in causing inhibition of spontaneously active vascular smooth muscle than myocardium in vitro.[2] Felodipine (10 µM) inhibits L-type Ca2+ channels by 30 to 65%??hereas scarcely blocks N- and P/Q-type Ca2+ channels.[3] Felodipine is exerts a markedly selective inhibition of the smooth muscle of arterial resistance vessels in vitro and in vivo.[4] Oral administration of felodipine is first metabolized in the gastrointestinal tract and liver by the enzyme CYP3A4.[1] In the rat and dog, the bioavailability of an oral dose for felodipine is about 15% because of high first-pass metabolism.[5]

References

[1] Silver PJ, et al. Effects of felodipine, nitrendipine and W-7 on arterial myosin phosphorylation, actin-myosin interactions and contraction. Eur J Pharmacol. 1984, 102(3-4): 417-424.
[2] Ljung B, et al. Pharmacodynamic properties of felodipine. Drugs. 1987, 34 Suppl 3: 7-15.
[3] Furukawa T, et al. Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes. J Pharmacol Exp Ther. 1999, 291(2): 464-473.
[4] Ljung B, et al. Felodipine sensitivity in vivo and in vitro of activation pathways in vascular smooth muscles. J Cardiovasc Pharmacol. 1987, 10 Suppl 1: S89-95.
[5] Eriksson UG, et al. Stereoselective metabolism of felodipine in liver microsomes from rat, dog, and human. Drug Metab Dispos. 1991, 19(5): 889-894.

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