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 1.2µM 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.
1. Zünkler, B.J., et al. 2000. Br. J. Pharmacol. 130: 1571-1574. PMID: 10928959 2. Crumb, W.J., 2000. J. Pharmacol. Exp. Ther. 292: 261-264. PMID: 10604956
Soluble in chloroform, DMSO (100 nM), ethanol (25 nM), and water (0.001 g/100 ml) at 30° C.
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Crumb (PubMed ID 10604956) found that theCrumb (PubMed ID 10604956) found that the antihistamines loratadine and terfenadine show similar human cardiac K(+) channel-blocking effects that can lead to arrhythmias in the human heart. -SCBT Publication Review
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