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.