A selective iNOS inhibitor
L-NIL is a relatively selective inhibitor of iNOS. It exhibits IC50 values of 0.4-3.3 ?M for iNOS as opposed to 8-38 and 17-92 ?M for eNOS and nNOS, respectively.1,2,3 L-NIL effectively inhibits iNOS both in vitro and in vivo.4,5,3 L-NIL has been used to demonstrate a critical role for iNOS in the immune response to infection by the protozoan L. major.3,6
1.Moore, W.M., Webber, R.K., Jerome, G.M., et al.L-N6-(1-Iminoethyl)lysine: A selective inhibitor of inducible nitric oxide synthaseJ. Med. Chem.373886-3888(1994) 2.Grant, S.K., Green, B.G., Stiffey-Wilusz, J., et al.Structural requirements for human inducible nitric oxide synthase substrates and substrate analogue inhibitorsBiochemistry374174-4180(1998) 3.Stenger, S., Thuring, H., Rollinghoff, M., et al.L-N6-(1-iminoethyl)-lysine potently inhibits inducible nitric oxide synthase and is superior to NG-monomethyl-arginine in vitro and in vivoEur. J. Pharmacol.294(2-3)703-712(1995) 4.Budzi?ski, M., Misterek, K., Gumulka, W., et al.Inhibition of inducible nitric oxide synthase in persistent painLife Sci.66301-305(2000) 5.Faraci, W.S., Nagel, A.A., Verdries, K.A., et al.2-Amino-4-methylpyridine as a potent inhibitor of inducible NO synthase activity in vitro and in vivoBr. J. Pharmacol.1191101-1108(1996) 6.Diefenbach, A., Schindler, H., Donhauser, N., et al.Type 1 interferon (IFNα/β) and type 2 nitric oxide synthase regulate the innate immune response to a protozoan parasiteImmunity8(1)77-87(1998)
动态评分
0.0