Synonym: a-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
CAS Number: 50679-08-8
Empirical Formula (Hill Notation): C32H41NO2
Molecular Weigh:t 471.67
EC Number: 256-710-8
MDL number: MFCD00079622
PubChem Substance: 24277779
Biochem/physiol Actions
Terfenadine inhibits HERG (human ether-a-gogo-related gene) K+ channels. It also blocks the delayed rectifier potassium current (IK) of rat isolated ventricular myocytes with IC50 value of 5.96 µM.
Non-sedating second generation H1 histamine receptor antagonist. Mainly metabolized by Cyp3A4, 5, 7. Inhibits CYP2C8.
Preparation Note
250 mg of Terfenadine dissolves in 5ml of chloroform to yield a clear, colorless solution. Terfenadine is also soluble at 30° C in 0.1 M citric acid (1.1 mg/ml), water (0.01 mg/ml), methanol (37.5 mg/ml), hexane (0.34 mg/ml), ethanol (37.8 mg/ml), 1 M hydrochloric acid (0.12 mg/ml), and 0.1 M tartaric acid (0.45 mg/ml).
Application
Terfenadine has been used to study the role of histamine in itch related to proteinase-activated receptors (PARs) in mice. Terfenadine has also been used to block histamine receptor type 1 to study the pathogenesis of 2,4-dinitrobenzene sulfonic acid (DNBS)-induced ulcerative colitis in rats.