Fexofenadine is a histamine H1 receptor antagonist (Ki = 10 nM). It reverses contraction of isolated rat tracheal strips induced by acetyl-β-methylcholine . Fexofenadine inhibits expression of IL-8 in TNF-α-stimulated HCT116 and COLO 205 cells. Oral administration of fexofenadine (2 and 10 mg/kg) reduces severity of colitis and phospho-IκB kinase activation in a mouse model of colitis induced by dextran sulfate sodium (DSS; ).
화학적 성질
Off-White Crystalline Solid
용도
Fexofenadine hydrochloride is used as an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist.
일반 설명
Fexofenadine hydrochloride, (±)-4-[1-hydroxy-4-[4-(hydroxyldiphenylmethyl)- 1-piperinyl]butyl-α,α-dimethylbenzeneacetic acid (Allegra), occurs as a white to off-white crystalline powder that is freely soluble in methanol and ethanol, slightly soluble in chloroform and water, and insoluble in hexane. This compound is marketed as a racemate and exists as a zwitterion in aqueous media at physiological pH. Fexofenadine is a primary oxidative metabolite of terfenadine. Terfenadine was developed during a search for new butyrophenone antipsychotic drugs as evidenced by the presence of the N-phenylbutanol substituent. It also contains a diphenylmethyl-piperidine moiety analogous to that found in the piperazine antihistamines.
생물학적 활성
Fexofenadine hydrochloride is a selective histamine H1 receptor antagonist (pKi = 8.1). Active metabolite of Terfenadine that displays non-sedating antiallergic effects. Fexofenadine hydrochloride counteracts histamine mediated immune suppression and improves immunotherapy response.
