Abstract
Unfortunately, none of these compounds has high selectivity for these channels. Mibefradil has been marketed worldwide for the treatment of hypertension and angina for a short period before it was withdrawn due to its pharmacokinetic and pharma- codynamic interactions with some other drugs such as terfen- adine, astemizole, cisapride, cyclosporine, tricyclic antidepre- ssants. 4 Mibefradil binds to skeletal muscle L-type calcium channels and brain voltage-gated sodium channels with disso- ciation constants of 2.3 and 17 nM, respectively. 5 It also can block potassium and chloride channels. 6 Obviously, this makes it not an ideal tool for in vitro or in vivo studies on T-type channels. Therefore, more potent and selective blockers are required to study the fundamental function of T-type channel and the related pathophysiological diseases such as epilepsy, neuronal pain, hypertension, congestive heart failure, and can- cer. 7-8
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