Abstract
Our aim was to verify potency and selectiveness of two most widely used drugs regarded as NOS-2 inhibitors: L-N6-(1-iminoethyl)-lysine (L-NIL) and S-methylisothiourea sulphate (SMT). Thioglycolate-elicited rat peritoneal macrophages and coronary endothelium of isolated guinea pig heart were used as assay systems for NOS-2 and NOS-3, respectively. A non-selective NOS inhibitor, N(G)-nitro-L-arginine methyl ester (L-NAME) was used as a reference compound. We found that L-NIL but not SMT was a selective NOS-2 inhibitor. Interestingly, L-NAME displayed selectivity towards NOS-3.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Enzyme Inhibitors / pharmacology
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Female
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Guinea Pigs
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Isothiuronium / analogs & derivatives*
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Isothiuronium / pharmacology
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Lysine / analogs & derivatives*
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Lysine / pharmacology
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Macrophages / drug effects
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Macrophages / metabolism
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Male
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Myocardium / metabolism
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NG-Nitroarginine Methyl Ester / pharmacology
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Nitric Oxide Synthase / antagonists & inhibitors*
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Nitric Oxide Synthase / metabolism
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Nitric Oxide Synthase Type II
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Nitric Oxide Synthase Type III
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Rats
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Vasodilation / drug effects
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Vasodilation / physiology
Substances
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Enzyme Inhibitors
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N(6)-(1-iminoethyl)lysine
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Isothiuronium
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Nitric Oxide Synthase
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Nitric Oxide Synthase Type II
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Nitric Oxide Synthase Type III
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Nos2 protein, rat
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Nos3 protein, rat
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S-methylisothiopseudouronium
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Lysine
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NG-Nitroarginine Methyl Ester