Skip to main content

Large-Conductance, Ca2+-Activated K+ Channels: Function, Pharmacology and Drugs

Buy Article:

$55.00 plus tax (Refund Policy)

Because of the physiological role played by the hyperpolarisation process resulting from a K+ outflow, it is not surprising that compounds able to activate outward K+ channels are considered as promising drugs, with exciting perspectives for the treatment of several cardiovascular, respiratory, neurological and urological diseases.

Among the different and numerous K+ channel families, medicinal chemistry has focused its major interest onto two channel types: the ATP-sensitive channels (KATP) and the large conductance subtype (BK), that belongs to the wide family of calcium-activated K+channels. BK channels are almost ubiquitous and exhibit single channel conductance of 100-300 pS, a property which justifies the potent role of these channels in the control of the membrane potential. BK channels have been investigated as potential therapeutic targets for different neuropathies, because of their profound influence on the neuronal activity. Moreover, BK channels are expected to have applications for the therapy of cardiovascular diseases. A potent feed-back control of the vascular and non-vascular smooth muscle tone is mediated by these channels, whose activation can be promoted by both a rise of the intracellular free calcium concentration as well as a membrane depolarisation. Additionally, BK channel activation can also be induced by other factors, such as cAMP-mediated phosphorylation, Gproteins, GMP and cGMP. The aim of this paper is to give a concise overview of the biological and pharmacological properties and potential therapeutic applications of activators of BK channels present at the vascular level. The ”state of the art“ in the pharmaceutical development of natural and synthetic BKactivators, with a description of the lead chemical structures, will be also described.
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: bk-activator; bk-opener; ca activated k channel; large conductance

Document Type: Review Article

Publication date: 2002-07-01

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more