Home Neuronal Signaling Histamine Receptor inhibitor Fexofenadine HCl For research use only.

Fexofenadine HCl

Synonyms: MDL 16455A

Fexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM.

Fexofenadine HCl Chemical Structure

Fexofenadine HCl Chemical Structure

CAS No. 153439-40-8

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Fexofenadine HCl Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Fexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM.
Targets
Histamine H1 receptor [1]
246 nM
In vitro
In vitro 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. [1] 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. [2] 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. [3]
In Vivo
In vivo 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. [4] 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. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03796377 Completed
Drug Interaction Study
Insel Gruppe AG University Hospital Bern|Bayer
 February 13 2019 Phase 1
NCT03078777 Unknown status
Hemodialysis
Lawson Health Research Institute
 November 29 2017 Phase 4

Chemical Information & Solubility

Molecular Weight 538.12 Formula

C32H39NO4.HCl
CAS No. 153439-40-8 SDF Download Fexofenadine HCl SDF
Smiles CC(C)(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)C(=O)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 107 mg/mL ( (198.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 107 mg/mL

Water : 2 mg/mL


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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