3557. Emedastine

Nomenclature

CAS number: 87233-61-2
1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole; 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole.
C17H26N4O; mol wt 302.41.
C 67.52%, H 8.67%, N 18.53%, O 5.29%.

Description and references

Histamine H1-receptor antagonist. Prepn: R. Iemura et al., EP 79545; eidem, US 4430343 (1983, 1984 both to Kanebo); eidem, J. Med. Chem. 29, 1178 (1986). GC determn in plasma: T. Hamada et al., Chem. Pharm. Bull. 34, 1168 (1986). Series of articles on pharmacology: Arzneim.-Forsch. 34, 801-818 (1984). Toxicity data: T. Fukuda et al., ibid. 801.

Chemical structure

Derivative

Difumarate.

Nomenclature

CAS number: 87233-62-3
KB-2413; LY-188695; Emadine (Alcon).
C17H26N4O.2C4H4O4; mol wt 534.56.
C 56.17%, H 6.41%, N 10.48%, O 26.94%.

Properties

Crystals from ethanol, mp 148-151°. LD50 orally in guinea pigs: 744 mg/kg (Fukuda).

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic