Jpn. J. Pharmacol. 85 (4), 339-350 (2001)

Molecular Pharmacology of T-type Ca2+ Channels

Tiffany N. Heady1, Juan C. Gomora2, Timothy L. Macdonald1 and Edward Perez-Reyes2,*

1Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA
2Department of Pharmacology, University of Virginia, Charlottesville, Virginia 22908, USA

*Corresponding author. FAX: +1-804-982-3878, E-mail:

Abstract: Over the past few years increasing attention has been focused on T-type calcium channels and their possible physiological and pathophysiological roles. Efforts toward elucidating the exact role(s) of these calcium channels have been hampered by the lack of T-type specific antagonists, resulting in the subsequent use of less selective calcium channel antagonists. In addition, the activity of these blockers often varies with cell or tissue type, as well as recording conditions. This review summarizes a variety of compounds that exhibit varying degrees of blocking activity towards T-type Ca2+ channels. It is designed as an aid for researchers in need of antagonists to study the biophysical and pathological nature of T-type channels, as well as a starting point for those attempting to develop potent and selective antagonists of the channel.

Keywords: T-type calcium channel, Antihypertensive, Mibefradil, Antiepileptic, Anesthetic, Antipsychotic, Amiloride
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