NDLI: Pharmacological profile of SL 59.1227, a novel inhibitor of the sodium/hydrogen exchanger

Content Provider	PubMed Central
Author	Lorrain, Janine Briand, Véronique Favennec, Evelyne Duval, Nicole Grosset, Alain Janiak, Philip Hoornaert, Christian Cremer, Gérard Latham, Christopher O'connor, Stephen E.
Copyright Year	2000
Abstract	The NHE1 isoform of the Na+/H+ exchanger plays an important role in the regulation of intracellular pH and in cardiac cell injury caused by ischaemia and reperfusion. SL 59.1227 is a novel imidazolypiperidine Na+/H+ antiport inhibitor which is structurally unrelated to previously described acylguanidine inhibitors such as cariporide. Recovery of pHi following an intracellular acid load was measured in CCL39-derived PS120 variant cells, selectively expressing either NHE1 or NHE2 isoforms of the Na+/H+ exchanger. pHi recovery was potently and selectively slowed by SL 59.1227 in NHE1-expressing cells (IC50 3.3±1.3 nM) versus NHE2-expressing cells (2.3±1.0 μM). The respective IC50 values for cariporide were 103±28 nM (NHE1) and 73±46 μM (NHE2). In anaesthetized rats following left coronary artery occlusion (7 min) and reperfusion (10 min) SL 59.1227 (10–100 μg kg−1 min−1 i.v.) inhibited ischaemia-mediated ventricular tachycardia (71–100%) and reperfusion-induced ventricular fibrillation (75–87%) and prevented mortality. Bolus i.v. administration of SL 59.1227 (1 mg kg−1) produced anti-arrhythmic effects when administered either before or during ischaemia. Cardiac infarct size was determined in anaesthetized rabbits following left coronary artery occlusion (30 min) and reperfusion (120 min). Infarct size measured as a percentage of the area at risk was 36.2±3.4% (control group) versus 15.3±3.9% (SL 59.1227 0.6 mg kg−1 i.v.). SL 59.1227 is the first example of a potent and NHE1-selective non-acylguanidine Na+/H+ exchanger inhibitor. It possesses marked cardioprotective properties.
Related Links	http://dx.doi.org/10.1038/sj.bjp.0703671
Ending Page	1194
Page Count	7
Starting Page	1188
File Format	PDF
ISSN	00071188
Journal	British Journal of Pharmacology
Issue Number	6
Volume Number	131
Language	English
Publisher Date	2000-11-01
Access Restriction	Open
Subject Keyword	Pharmacology Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Pharmacology

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