Skip Navigation

European Heart Journal 1991 12(Supplement F):30-37; doi:10.1093/eurheartj/12.suppl_F.30
Copyright © 1991 by the European Society of Cardiology.
This Article
Right arrow Full Text (PDF)
Right arrow E-letters: Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when E-letters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrowRequest Permissions
Right arrow Disclaimer
Google Scholar
Right arrow Articles by Carmeliet, E.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Carmeliet, E.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

© 1991 The European Society of Cardiology

Ion channel agonists: expectations for therapy

E. Carmeliet

Laboratory of Physiology, University of Leuven Campus Gasthuisberg, Herestraat, 49, 3000 Leuven, Belgium

Correspondence: Dr E. Carmeliet, Laboratory of Physiology, University of Leuven, Campus Gasthuisberg, Herestraat, 49, 3000 Leuven, Belgium

Some animal or plant toxins and man-made drugs exert agonist activity on Na+, Ca2+ and K+ channels. The increase in current through these channels is essentially due to an increase of ‘open probability’ and not of single channel conductance. The enhanced open probability is caused by a prolongation of the open time. In the case of voltage-operated channels this change in open time can be accompanied by increased reopenings and thus slowing of inactivation, or a shift in the activation process to more negative potentials. In the case of the ligand-operated K+ channel, a decrease in the affinity for the normal physiological ligand, ATP, is the mechanism underlying the enhancement of open probability.

Agonists show potential clinical applications for Na+ and Ca2+ channels more specifically as positive inotropic agents in cardiac tissue. For K+ channels, the potential therapeutic field is even broader and spans from relaxation of smooth muscle (hypertension, asthma, bladder, uterus), reduction in excitability (arrhythmias, certain skeletal muscle myopathies) to inhibition of neurotransmitter release (depression, epilepsy).

Key Words: Ion channels • agonist • antagonist


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?




Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.