In vitro and in vivo pharmacology of a structurally novel Na+‐H+ exchange inhibitor, T‐162559

We investigated the inhibitory effects of a non‐acylguanidine Na+‐H+ exchange (NHE) inhibitor, T‐162559 ((5E,7S)‐[7‐(5‐fluoro‐2‐methylphenyl)‐4‐methyl‐7,8‐dihydro‐5(6H)‐quinolinylideneamino] guanidine dimethanesulphonate), on NHE‐1, and its cardioprotective effect against ischaemia and reperfusion i...

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Veröffentlicht in:	British journal of pharmacology 2002-04, Vol.135 (8), p.1995-2003
Hauptverfasser:	Kusumoto, Keiji, Igata, Hideki, Abe, Akemi, Ikeda, Shota, Tsuboi, Ayako, Imamiya, Eikoh, Fukumoto, Shoji, Shiraishi, Mitsuru, Watanabe, Toshifumi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Blood Platelets - drug effects Blood Platelets - metabolism cardioprotection Cardiotonic Agents - administration & dosage Cardiotonic Agents - pharmacology Cardiovascular system cariporide Dose-Response Relationship, Drug eniporide Guanidines - administration & dosage Guanidines - chemistry Guanidines - pharmacology Humans In Vitro Techniques Injections, Intravenous ischaemia‐reperfusion Male Medical sciences Miscellaneous myocardial infarction Myocardial Infarction - pathology Myocardial Infarction - prevention & control Myocardial Ischemia - drug therapy Myocardial Reperfusion Injury - drug therapy Na+‐H+ exchanger Pharmacology. Drug treatments Quinolines - administration & dosage Quinolines - chemistry Quinolines - pharmacology Rabbits Rats Rats, Wistar Sodium-Hydrogen Exchangers - antagonists & inhibitors Sulfones - pharmacology
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Zusammenfassung:	We investigated the inhibitory effects of a non‐acylguanidine Na+‐H+ exchange (NHE) inhibitor, T‐162559 ((5E,7S)‐[7‐(5‐fluoro‐2‐methylphenyl)‐4‐methyl‐7,8‐dihydro‐5(6H)‐quinolinylideneamino] guanidine dimethanesulphonate), on NHE‐1, and its cardioprotective effect against ischaemia and reperfusion injury in rats and rabbits. T‐162559 inhibited human platelet NHE‐1 in a concentration‐dependent manner, with an IC50 value of 13±3 nmol l−1, making it 16 and three times more potent than cariporide IC50: 209±75 nmol l−1, P
ISSN:	0007-1188 1476-5381
DOI:	10.1038/sj.bjp.0704647