2275. Cilnidipine

Nomenclature

CAS number: 132203-70-4
1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl (2E)-3-phenyl-2-propenyl ester; (±)-(E)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate; FRC-8653; Atelec (Morishita); Cinalong (Fujirebio); Siscard (Boehringer, Ing.).
C27H28N2O7; mol wt 492.52.
C 65.84%, H 5.73%, N 5.69%, O 22.74%.

Description and references

Dihydropyridine calcium channel blocker. Prepn: T. Kutsuma et al., EP 161877; eidem, US 4672068 (1985, 1987 both to Fujirebio). Pharmacology: K. Ikeda et al., Oyo Yakuri 44, 433 (1992). Mechanism of action study: M. Hosono et al., J. Pharmacobio-Dyn. 15, 547 (1992). LC-MS determn in plasma: K. Hatada et al., J. Chromatogr. 583, 116 (1992). Clinical study: M. Ishii, Jpn. Pharmacol. Ther. 21, 59 (1993). Acute toxicity study: S. Wada et al., Yakuri to Chiryo 20, Suppl. 7, S1683 (1992), C.A. 118, 32711 (1992).

Chemical structure

Properties

Crystals from methanol, mp 115.5-116.6°. LD50 in male, female mice, rats (mg/kg): ≥5000, ≥5000, ≥5000, 4412 orally; ≥5000 all species s.c.; 1845, 2353, 441, 426 i.p. (Wada).

Therapeutic Category

Antihypertensive.

Keywords

Antihypertensive; Dihydropyridine Derivatives; Calcium Channel Blocker; Dihydropyridine Derivatives