Abstract:
:Terfenadine and astemizole rarely cause cardiac arrhythmias by suppressing the cardiac rapid delayed rectifier K+ channel encoded by the human ether-a-go-go-related gene (HERG). Epinastine, however, has not been reported to have the adverse effect. We have therefore compared the effects of epinastine, terfenadine and astemizole on HERG channels expressed in Xenopus oocytes. Terfenadine and astemizole suppressed the HERG current with IC50 of 431 nM and 69 nM, respectively. In contrast, 100 microM epinastine inhibited the HERG current by only 11+/-2.1%. These results may provide an explanation for the difference in the cardiotoxicity between different nonsedating histamine H1 receptor antagonists.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Chachin M,Katayama Y,Yamada M,Horio Y,Ohmura T,Kitagawa H,Uchida S,Kurachi Ydoi
10.1016/s0014-2999(99)00375-1keywords:
subject
Has Abstractpub_date
1999-06-25 00:00:00pages
457-60issue
3eissn
0014-2999issn
1879-0712pii
S0014-2999(99)00375-1journal_volume
374pub_type
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