L-N6-(1-iminoethyl)-lysine (L-NIL) but not S-methylisothiourea sulphate (SMT) displays selectivity towards NOS-2.
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.
Chłopicki
S
S
Department of Pharmacology, Jagiellonian University, Medical College, Kraków, Poland.
Olszanecki
R
R
Jakubowski
A
A
Lomnicka
M
M
Gryglewski
R J
RJ
D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D007550:Isothiuronium / Q000031:analogs & derivatives* / Q000494:pharmacology; D008239:Lysine / Q000031:analogs & derivatives* / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008297:Male; D009206:Myocardium / Q000378:metabolism; D019331:NG-Nitroarginine Methyl Ester / Q000494:pharmacology; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D052247:Nitric Oxide Synthase Type II; D052250:Nitric Oxide Synthase Type III; D051381:Rats; D014664:Vasodilation / Q000187:drug effects / Q000502:physiology
D004791:Enzyme Inhibitors; C090663:N(6)-(1-iminoethyl)lysine; D007550:Isothiuronium; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; D052250:Nitric Oxide Synthase Type III; C496318:Nos2 protein, rat; C496316:Nos3 protein, rat; C027744:S-methylisothiopseudouronium; D008239:Lysine; D019331:NG-Nitroarginine Methyl Ester