felodipine-d5 Chemical Properties

storage temp. 

Store at -20°C

solubility 

Chloroform: soluble

form 

A solid

felodipine-d5 Usage And Synthesis

Description

(±)-Felodipine-d₅ 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 (EC₅₀ = 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 (IC₅₀ = 6.8 μM). (±)-Felodipine preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC₅₀s = 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.

Uses

Felodipine-d5 is the labeled analogue of Felodipine (F232375), a dihydropyridine calcium channel blocker.

References

[1] T FURUKAWA. Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes.[J]. Journal of Pharmacology and Experimental Therapeutics, 1999, 291 2: 464-473.
[2] J D JOHNSON  D A F. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments.[J]. Journal of Pharmacology and Experimental Therapeutics, 1983, 226 2: 330-334.
[3] EDWARD PEREZ-REYES I V Amy L Van Deusen. Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs.[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328 1: 621-627. DOI: 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