Fexofenadine Hydrochloride153439-40-8盐酸非索非那定

Fexofenadine Hydrochloride153439-40-8盐酸非索非那定

盐酸非索非那定
分子式：C32H39NO4.HCl    分子量：538.13
 
产品描述
Fexofenadine抑制histamine H1受体，IC50为246 nM。
靶点
Histamine H1
         
IC50
246 nM
         
体外研究
Fexofenadine exhibits a potent and concentration-dependent anti-anaphylactic activity with an IC50 value of 95.5nM. Fexofenadine shows only a weak competitive antagonist behaviour for the 5-HT2A receptorsfrom rat caudal artery with pA2 of 5.2.All four P-gp inhibitors has a strong, concentration-dependent effect on the Papp of fexofenadine in both directions in the Caco-2 cell model. The IC50 of verapamil is 8.44 mM on the P-gp-mediated secretion of Fexofenadine.Fexofenadine causes a significant increase in the QT and Tp-e intervals and receives a significant TdP score at doses greater than 100 fold its free TPC in the rabbit left ventricular wedge preparation.
体内研究
Fexofenadine is excreted unchanged in the urine, bile, and gastrointestinal tract, indicating minimal metabolism in rats, making it an ideal probe to study transport processes. Coadministration of Fexofenadine with Ketoconazole increases the oral exposure of Fexofenadine by 187% in rats. In contrast, coadministration of Fexofenadine with orange juice or apple juice to rats decreases the oral exposure of Fexofenadine by 31% and 22%, respectively. Increasing the quantity of orange or apple juice administered further decreases the oral exposure of Fexofenadine, by 40% and 28%, respectively.Biliary excretion clearance of Fexofenadine (17 ml/min/kg) accounts for almost 60% of the total body clearance (30 ml/min/kg) in mice. Knockout mice of Mdr1a/1b P-gp does not affect the biliary excretion clearance with regard to both plasma and liver concentrations, whereas the absence of P-gp causes a 6-fold increase in the plasma concentration and 3-fold higher brain-to-plasma concentration ratio after oral administration.
溶解性
DMSO 107 mg/mL，水 2 mg/mL，乙醇 107 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO