Bioactivity | Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3]. | ||||||||||||
Invitro | Felodipine, a dihydropyridine calcium antagonist, is the most potent in relaxing porcine coronary arteries (IC50=0.15 nM)[1]. Felodipine, an L-type calcium channel blocker, induces autophagy and clears diverse aggregate-prone, neurodegenerative disease-associated proteins [2]. Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM[3]. | ||||||||||||
Name | Felodipine | ||||||||||||
CAS | 72509-76-3 | ||||||||||||
Formula | C18H19Cl2NO4 | ||||||||||||
Molar Mass | 384.25 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Johnson JD, et al. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther. 1983;226(2):330-334. [2]. Siddiqi FH, et al. Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing [published correction appears in Nat Commun. 2019 Jun 4;10(1):2530]. Nat Commun. 2019;10(1):1817. Published 2019 Apr 18. [3]. Yiu, S. and E.E. Knaus, Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem, 1996. 39(23): p. 4576-82. |