Description
(±)-Felodipine-d
5 is intended for use as an internal standard for the quantification of (±)-felodipine by GC- or LC-MS. (±)-Felodipine is an inhibitor of L-type calcium channels. It induces relaxation of precontracted isolated porcine coronary artery segments (EC
50 = 0.15 nM), which highly express L-type calcium channels. (±)-Felodipine is selective for L-type calcium channels over N-, R-, and P/Q-type channels at 10 μM, as well as the T-type Ca
v3.2 channel (IC
50 = 6.8 μM). (±)-Felodipine preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC
50s = 33.9 and 3,981 nM, respectively). It decreases mean arterial blood pressure and total peripheral resistance in a rabbit model of hypertension induced by renal artery ligation when administered intravenously at doses of 30 and 100 nmol/kg.
References
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10.1124/jpet.108.145672[4] LJUNG B. Vascular selectivity of felodipine: experimental pharmacology.[J]. Journal of Cardiovascular Pharmacology, 1990, 15 Suppl 4: S11-6. DOI:
10.1097/00005344-199015004-00003[5] G R BOLT P R S. Acute systemic and regional hemodynamic effects of felodipine, a new calcium antagonist, in conscious renal hypertensive rabbits.[J]. Journal of Cardiovascular Pharmacology, 1984, 6 4: 707-712. DOI:
10.1097/00005344-198407000-00025
