TABLE 1

Nonselective inhibitors of nitric-oxide synthase isoforms The values of IC50 and Ki are calculated on binding studies to the relative isotype selectivity of the inhibitor. These values depend upon the exact system used for the measurement (see References).

NOS-I NOS-II NOS-III References
Inhibitors of NOS-I (nNOS)
   5-Ethyl-N-[4-trifluoro(methyl)phenyl]-isothiourea K i 0.32 μM 37 μM 9.4 μM Wolff et al., 1994
   α-Fuanidinoglutaric acid Shearer et al., 1997
   l-N5-(1-Iminoethyl)-ornithine (l-NIO) K i 1.7 μM 3.9 μM 3.9 μM Yokoi et al., 1994
   N5-(1-Imino-3-butenyl)-l-ornitine K i 0.1 μM 60 μM 12 μM Furfine et al., 1994
   7-Nitroindazole IC50 0.71 μM 0.80 μM Rees et al., 1990
   3-Bromo-7-nitroindazole IC50 170 nM ≈200 nM Babbedge et al., 1993
   Nω[ρ]-Propyl-l-arginine K i 0.057 μM 180 μM 8.5 μM Zhang et al., 1997
   l-Thiocitrulline K i 0.06 μM 3.6 μM Furfine et al., 1994
   S-Methyl-l-thiocitrulline IC50 0.3 μM 5.4 μM Handy et al., 1936
   1-(2-Trifluoromethylphenyl)imidazole IC50 28.2 μM 27.0 μM 1.06 mM Babu and Griffith, 1998a
Inhibitors of NOS-II (iNOS)
   S-Methyl-isothiourea K i 6 μM Webber et al., 1998
   S-(2-Aminoethyl)-isothiourea K i 6 μM Garvey et al., 1994
   2-Imino-4-methylpiperidine IC50 0.2 μM 0.1 μM 1.1 μM Griffiths et al., 1993
   Aminoguanidine K i 157 μM 75 μM Garvey et al., 1994
   l-N5-(1-Iminoethyl)-ornithine (l-NIO) K i 1.7 μM 3.9 μM 3.9 μM Rees et al., 1990
   l-Thiocitrulline K i 0.06 μM 3.6 μM Furfine et al., 1994
Inhibitors of NOS-III (eNOS)
   S-Ethyl-isothiourea K i 0.029 μM 0.017 μM 0.036 μM Nakane et al., 1995
   S-Isopropyl-ITU K i 0.01 μM Rees et al., 1990
   l-N5-(1-Iminoethyl)-ornithine (l-NIO) K i 1.7 μM 3.9 μM 3.9 μM Southan et al., 1995