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

Ralf Köhler, Brajesh P. Kaistha, Heike Wulff

Research output: Contribution to journalArticlepeer-review

78 Scopus citations


Importance of the field: Cardiovascular disease is a leading cause of death in modern societies. Hyperpolarizing Ca2+-activated K+ channels (KCa) 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 KCa 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-factormediated 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 KCa 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.

Original languageEnglish (US)
Pages (from-to)143-155
Number of pages13
JournalExpert Opinion on Therapeutic Targets
Issue number2
StatePublished - Feb 2010


  • Antihypertensives
  • Ca-activated K channels
  • EDHF
  • Hypertension
  • KCa2.3
  • KCa3.1
  • Restenosis

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Clinical Biochemistry
  • Molecular Medicine


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