Abstract
LAS 31180 (3-methylsulphonylamino-1-methyl-4(1H)-quinolone, CAS 137338-43-3) was found to have positive inotropic and vasodilator properties through its inhibitory action on type 3 phosphodiesterase. The inotropic effects of LAS 31180 were demonstrated in vitro both in isolated guinea-pig ventricular strips (EC50 of 1.2 mumol/l) and in isolated guinea-pig working hearts. In conscious chronically instrumented Beagle dogs, LAS 31180 administered either by intravenous or oral route, showed a dose-dependent, long-lasting positive inotropic effect with minimal effects on heart rate. In hypertensive Beagle dogs LAS 31180 elicited a potent and long-lasting fall in blood pressure.
MeSH terms
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Administration, Oral
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Animals
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Antihypertensive Agents / pharmacology
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Cardiotonic Agents / pharmacology*
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Dogs
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Dose-Response Relationship, Drug
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Guinea Pigs
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Heart Ventricles / drug effects
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In Vitro Techniques
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Injections, Intravenous
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Isoenzymes / antagonists & inhibitors
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Male
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Mice
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Myocardial Contraction / drug effects
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Phosphodiesterase Inhibitors / pharmacology
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Phosphoric Diester Hydrolases / metabolism
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Quinolones / pharmacology
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Sulfonamides / pharmacology
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Vasodilator Agents / pharmacology*
Substances
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Antihypertensive Agents
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Cardiotonic Agents
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Isoenzymes
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Phosphodiesterase Inhibitors
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Quinolones
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Sulfonamides
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Vasodilator Agents
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LAS 31180
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Phosphoric Diester Hydrolases