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Expert Opin Ther Targets. 2010 Feb;14(2):143-55. doi: 10.1517/14728220903540257.

Vascular KCa-channels as therapeutic targets in hypertension and restenosis disease.

Author information

1
Institute of Medical Biology, Depatrment of Physiology, SDU, J.B. Winsløwsvej 21 3., 5000 Odense C, Denmark. rkohler@health.sdu.dk

Abstract

IMPORTANCE OF THE FIELD:

Cardiovascular disease is a leading cause of death in modern societies. Hyperpolarizing Ca(2+)-activated K(+) channels (K(Ca)) are important membrane proteins in the control of arterial tone and pathological vascular remodelling and thus could serve as new drug targets.

AREAS COVERED IN THIS REVIEW:

We summarize recent advances in the field of vascular K(Ca) and their roles in cardiovascular pathologies such as hypertension and restenosis disease and draw attention to novel small-molecule channel modulators and their possible therapeutic utility. This review focuses on literature from the last four to five years.

WHAT THE READER WILL GAIN:

Pharmacological opening of endothelial KCa3.1/KCa2.3 channels stimulates endothelium-derived-hyperpolarizing-factor-mediated arteriolar dilation and lowers blood pressure. Inhibition of smooth muscle KCa3.1 channels has beneficial effects in restenosis disease and atherosclerosis. We consider the therapeutic potential of KCa3.1/KCa2.3 openers as novel endothelium-specific antihypertensive drugs as well as of KCa3.1-blockers for the treatment of pathological vascular remodelling and discuss advantages and disadvantages of the pharmacotherapeutic approaches.

TAKE HOME MESSAGE:

Pharmacological manipulation of vascular K(Ca) channels by novel small-molecule modulators offers new venues for alternative treatments of hypertension, restenosis and atherosclerosis. Additional efforts are required to optimize these compounds and to validate them as cardiovascular-protective drugs.

PMID:
20055714
PMCID:
PMC3644209
DOI:
10.1517/14728220903540257
[Indexed for MEDLINE]
Free PMC Article

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