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(Circulation Research. 2009;105:112.)
© 2009 American Heart Association, Inc.

Editorials

L-Type Calcium Channel Antagonists and Suppression of Expression of Plasminogen Receptors

Is the Missing Link the L-Type Calcium Channel?

Ghassan Bkaily, Danielle Jacques

From the Department of Anatomy and Cell Biology, Faculty of Medicine, University of Sherbrooke, Quebec, Canada.

Correspondence to Dr G. Bkaily, Department of Anatomy and Cell Biology, Faculty of Medicine, University of Sherbrooke, Quebec, Canada, J1H 5N4. E-mail Ghassan.Bkaily@Usherbrooke.ca

See related article, pages 167–175

Key Words: L-type calcium channel • calcium • calcium antagonists • Plg receptors • macrophage

An extract of the first 250 words of the full text is provided, because this article has no abstract.

Several types of voltage-dependent Ca²⁺ channels were reported in many excitable and nonexcitable cell types, including the L-, T-, P-, N-, and Q-types; the isradipine sensitive steady-state resting R-type^1,2; and the nifedipine resistant R-type channels.³ The presence of some of these voltage-dependent Ca²⁺ channel types depends on cell origin. Among these channels, the L-type is the most studied channel because of the large number of Ca²⁺ blockers that affect its function. Historically, calcium channel antagonists were developed before the discovery of the L-type Ca²⁺ channel. These Ca²⁺ channel antagonists are divided into 3 classes of drugs: benzothiazepines (such as verapamil), dihydropyridines (such as amlodipine), and phenylalkylamines (such as diltiazem). The 3 classes of L-type Ca²⁺ channel antagonists have different relative selectivity for cardiac and vascular tissues. Their effects depend on the frequency of channel opening and where they physically bind on the channel.

L-type Ca²⁺ channel antagonists have been studied for many years in other fields of application other than blockade of calcium entry through the L-type voltage-dependent Ca²⁺ channel. Historically, the literature in the field of L-type Ca²⁺ channel blockers is full of information concerning their effects on other sites that regulate Ca²⁺ movements into and within cells. Among these effects are blockade of Ca²⁺ pumps,⁴ Na⁺/Ca²⁺ exchange,^4–7 Na⁺/K⁺ pump,^4–7 protein kinase C,⁹ and mitochondrial respiration. These L-type Ca²⁺ channel blockers were reported to act as antihypertensive, antianginal, antiarrhythmic, and antiplatelet agents. In addition, they were also reported to possess both immunosuppressive¹⁰ and antiinflammatory activity. The . . . [Full Text of this Article]

Related Article:

L-Type Calcium Channel Blockers Exert an Antiinflammatory Effect by Suppressing Expression of Plasminogen Receptors on Macrophages

Riku Das, Tim Burke, David R. Van Wagoner, and Edward F. Plow
Circ. Res. 2009 105: 167-175. [Abstract] [Full Text] [PDF]