3484. Ebastine

Nomenclature

CAS number: 90729-43-4
1-[4-(1,1-Dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone; 4′-tert-butyl-4-[4-(diphenylmethoxy)piperidino]butyrophenone; 4-diphenylmethoxy-1-[3-(4-tert-butylbenzoyl)propyl]piperidine; LAS-W-090; Ebastel (Almirall); Estivan (Almirall); Evastel (Almirall); Kestin (Almirall); Kestine (Almirall).
C32H39NO2; mol wt 469.66.
C 81.83%, H 8.37%, N 2.98%, O 6.81%.

Description and references

Nonsedating type histamine H1-receptor antagonist. Prepn: J. M. P. Soto et al., EP 134124; eidem, US 4550116 (both 1985 to Fordonal). Metabolized in vivo to carebastine, its active carboxylic acid metabolite. Clinical pharmacology, pharmacokinetics: J. Vincent et al., Br. J. Clin. Pharmacol. 26, 497 (1988). Effect on psychomotor performance: J. Vincent et al., ibid. 503.

Chemical structure

Derivative

Fumarate.
C32H39NO2.C4H4O4; mol wt 585.73.
C 73.82%, H 7.40%, N 2.39%, O 16.39%.

Properties

Crystals from ethanol, mp 197-198°.

Therapeutic Category

Antihistaminic.

Keywords

Antihistaminic