Article: Inhibition of late sodium current to reduce electrical and mechanical dysfunction of ischaemic myocardium.
British journal of pharmacology
2007 Volume 153, Issue 6, Page(s) 1128–1132
Abstract: This commentary on the review by DA Saint in the current issue of the British Journal of Pharmacology focuses on the pathological role of late I(Na) in the heart, the evidence supporting inhibition of late I(Na) as a therapeutic target in ischaemic heart ...
Abstract | This commentary on the review by DA Saint in the current issue of the British Journal of Pharmacology focuses on the pathological role of late I(Na) in the heart, the evidence supporting inhibition of late I(Na) as a therapeutic target in ischaemic heart disease, and the therapeutic applications and challenges for development of new late I(Na) inhibitors. Recent reports from a large clinical outcome trial (MERLIN) of ranolazine, a drug known to inhibit late I(Na), indicated that it was safe and reduced recurrent ischaemia and arrhythmic activity. In combination with other results indicating that inhibition of late I(Na) reduces ischaemia, myocardial Ca(2+) overload, and electrical and mechanical dysfunction when late I(Na) is increased, the new clinical trial results suggest that reduction of cardiac late I(Na) is safe and therapeutically beneficial. |
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MeSH term(s) | Acetanilides/pharmacology ; Animals ; Calcium/metabolism ; Controlled Clinical Trials as Topic ; Drug Delivery Systems ; Drug Design ; Electrophysiology ; Enzyme Inhibitors/pharmacology ; Humans ; Myocardial Ischemia/drug therapy ; Myocardial Ischemia/physiopathology ; Piperazines/pharmacology ; Ranolazine ; Sodium Channel Blockers/pharmacology ; Sodium Channels/drug effects ; Sodium Channels/metabolism |
Chemical Substances | Acetanilides ; Enzyme Inhibitors ; Piperazines ; Sodium Channel Blockers ; Sodium Channels ; Ranolazine (A6IEZ5M406) ; Calcium (SY7Q814VUP) |
Language | English |
Publishing date | 2007-12-10 |
Publishing country | England |
Document type | Comment ; Journal Article |
ZDB-ID | 80081-8 |
ISSN | 1476-5381 ; 0007-1188 |
ISSN (online) | 1476-5381 |
ISSN | 0007-1188 |
DOI | 10.1038/sj.bjp.0707522 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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