Molecular structure of Terfenadine, CAS Number: 50679-08-8
Terfenadine (CAS 50679-08-8)
Alternate Names:
α-[4-(1,1-Dmethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Application:
Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KIR6 channels
CAS Number:
50679-08-8
Molecular Weight:
471.67
Molecular Formula:
C32H41NO2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KIR6 (KATP) channels. The IC values for Terfenadines inhibitory activity against these channels is 204nM for HERG and 1.2microM for KIR6 (KATP). Studies show that Terfenadine inhibits the delayed rectifier K+ in ventricular myocytes. Terfenadine is converted into its more active form, terfenadine carboxylate by the enzyme CYP3A4. Terfenadine is an inhibitor of CYP2C8.
Terfenadine (CAS 50679-08-8) References
- Pregnancy outcome after gestational exposure to terfenadine: A multicenter, prospective controlled study. | Loebstein, R., et al. 1999. J Allergy Clin Immunol. 104: 953-6. PMID: 10550738
- Loratadine blockade of K(+) channels in human heart: comparison with terfenadine under physiological conditions. | Crumb, WJ. 2000. J Pharmacol Exp Ther. 292: 261-4. PMID: 10604956
- Mechanism of terfenadine block of ATP-sensitive K(+) channels. | Zünkler, BJ., et al. 2000. Br J Pharmacol. 130: 1571-4. PMID: 10928959
- Terfenadine-beta-Cyclodextrin inclusion complex with antihistaminic activity enhancement. | Choi, HG., et al. 2001. Drug Dev Ind Pharm. 27: 857-62. PMID: 11699838
- Evaluation of terfenadine and ketoconazole-induced QT prolongation in conscious telemetered guinea pigs. | Rajput, SK., et al. 2010. Pharmacol Rep. 62: 683-8. PMID: 20885008
- Distribution of terfenadine and its metabolites in locusts studied by desorption electrospray ionization mass spectrometry imaging. | Olsen, LR., et al. 2015. Anal Bioanal Chem. 407: 2149-58. PMID: 25404166
- Comparison of electropharmacological effects between terfenadine and its active derivative fexofenadine using a cross-over study in halothane-anesthetized dogs to analyze variability of pharmacodynamic and pharmacokinetic profiles of terfenadine and torsadogenic risk of fexofenadine. | Ando, K., et al. 2018. J Toxicol Sci. 43: 183-192. PMID: 29540652
- Molecular Mobility of Terfenadine: Investigation by Dielectric Relaxation Spectroscopy and Molecular Dynamics Simulation. | Dudognon, E., et al. 2019. Mol Pharm. 16: 4711-4724. PMID: 31589458
- Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels. | Delgado-Ramírez, M., et al. 2021. Acta Pharm. 71: 317-324. PMID: 33151169
- Terfenadine increases the QT interval in isolated guinea pig heart. | Pinney, SP., et al. 1995. J Cardiovasc Pharmacol. 25: 30-4. PMID: 7723350
- Possible interactions with terfenadine or astemizole. | Zechnich, AD., et al. 1994. West J Med. 160: 321-5. PMID: 8023479
- Itraconazole affects single-dose terfenadine pharmacokinetics and cardiac repolarization pharmacodynamics. | Honig, PK., et al. 1993. J Clin Pharmacol. 33: 1201-6. PMID: 8126255
- Effects of terfenadine and its metabolites on a delayed rectifier K+ channel cloned from human heart. | Rampe, D., et al. 1993. Mol Pharmacol. 44: 1240-5. PMID: 8264561
- Terfenadine-ketoconazole interaction. Pharmacokinetic and electrocardiographic consequences. | Honig, PK., et al. JAMA. 269: 1513-8. PMID: 8445813
- The cardiac effects of terfenadine after inhibition of its metabolism by grapefruit juice. | Clifford, CP., et al. 1997. Eur J Clin Pharmacol. 52: 311-5. PMID: 9248771
Inhibitor of:
ABCA4, ATP-binding cassette sub-family A (ABCA), CYP2C8, CYP2J11, CYP2J9, DDX43, E030010A14Rik, EAG, GSTO2, HERG, Histamine H1 Receptor, HPS-1, KCNE3, KCNH3, KCNH5, KCNH7, KIR, PABPC4, TREK-1, and TREK-2.Activator of:
CaM V, CYP2J9, KV9.2, MANSC4, and MaxiKβ.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Terfenadine, 500 mg | sc-208421A | 500 mg | $43.00 | |||
Terfenadine, 1 g | sc-208421B | 1 g | $70.00 | |||
Terfenadine, 5 g | sc-208421 | 5 g | $118.00 |