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: eperez@virginia.edu
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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