3953. Felodipine

Nomenclature

CAS number: 72509-76-3
4-(2,3-Dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl ester; H-154/82; Agon (TheraPharm); Feloday (Novartis); Flodil (AstraZeneca); Hydac (Aventis); Munobal (Aventis); Plendil (AstraZeneca); Prevex (Schering); Splendil (AstraZeneca).
C18H19Cl2NO4; mol wt 384.25.
C 56.26%, H 4.98%, Cl 18.45%, N 3.65%, O 16.66%.

Description and references

Dihydropyridine calcium channel blocker marketed as the racemate. Prepn: P. B. Berntsson et al., EP 7293; eidem, US 4264611 (1980, 1981 both to AB Hassle). Conformation: P. B. Berntsson, R. E. Carter, Acta Pharm. Suec. 18, 221 (1981). Interaction with calmodulin, q.v.: S. L. Bostr"om et al., Nature 292, 777 (1981). Diuretic-natriuretic properties: G. F. Dibona et al., Clin. Res. 30, 571A (1982). Hemodynamic effects in coronary patients: P. Decoster et al., Eur. J. Clin. Invest. 12, 43 (1982). Enantioselective determn in plasma: P. A. Soons et al., J. Chromatogr. 528, 343 (1990); HPLC-MS-MS determn in plasma: L. H. Miglioranca et al., J. Chromatogr. B 814, 217 (2005). Pharmacokinetics and pharmacodynamics: B. Edgar et al., Biopharm. Drug Dispos. 8, 235 (1987). Pharmacokinetics, vascular selectivity, effects on hypertension, hemodynamics and renal function: Drugs 29, Suppl. 2, 1-212 (1985).

Chemical structure

Properties

Crystals from isopropyl ether, mp 145°.

Therapeutic Category

Antihypertensive; antianginal.

Keywords

Antianginal; Antihypertensive; Dihydropyridine Derivatives; Calcium Channel Blocker; Dihydropyridine Derivatives