Pathophysiological significance of T-type Ca2+ channels: T-type Ca2+ channels and drug development.
T-type Ca(2+) channels are present in cardiovascular, neuronal, and endocrine systems; and they are now receiving attention as novel therapeutic targets. Many drugs and compounds non-specificaly block T-type Ca(2+) channels. Certain dihydropyridine compounds, such as efonidipine, have blocking activity on both L-type and T-type Ca(2+) channels which possibly underlies their excellent clinical profiles such as minimum reflex tachycardia and renal protection. Selective inhibitors of T-type Ca(2+) channels, such as non-hydrolyzable mibefradil and R(-)-efonidipine, are powerful pharmacological tools for further studies and may lead to the development of novel therapeutic strategies.
Tanaka
Hikaru
H
Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan. htanaka@phar.toho-u.ac.jp
Shigenobu
Koki
K
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020746:Calcium Channels, L-Type / Q000187:drug effects; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D004095:Dihydropyridines / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D020748:Mibefradil / Q000494:pharmacology; D009596:Nitrophenols / Q000494:pharmacology; D009943:Organophosphorus Compounds / Q000494:pharmacology
D002121:Calcium Channel Blockers; D020746:Calcium Channels, L-Type; D020747:Calcium Channels, T-Type; D004095:Dihydropyridines; D009596:Nitrophenols; D009943:Organophosphorus Compounds; D020748:Mibefradil; C066425:efonidipine