Table 2.
Compounds |
Ki (μM)a |
Selectivityb |
|||
---|---|---|---|---|---|
nNOS | eNOS | iNOS | n/e | n/i | |
L-NNAc | 0.57 | 0.75 | 4.55 | 1.3 | 8 |
(±)-8 | 47.94 | 121.62 | 609.43 | 2.5 | 13 |
(±)-9 | 3.98 | 172.91 | 437.76 | 43 | 110 |
(±)-10 | 304.96 | 849.21 | 2,522.8 | 3 | 8 |
(±)-11 | 13.47 | 1,696 | 651.85 | 126 | 48 |
(±)-12 | 6.94 | 340.83 | 25.24 | 49 | 4 |
(±)-13 | 15.68 | 241.7 | 308.1 | 15 | 20 |
(±)-14 | 14.45 | 2,906 | 166.1 | 201 | 11.5 |
(±)-15 | 13.86 | 1,453 | 298.55 | 105 | 21.5 |
(±)-16 | 20.57 | 1,453 | 416.61 | 71 | 20 |
(±)-17 | 12.85 | 625.42 | 234.06 | 49 | 18 |
(±)-18 | 20.93 | 460.16 | 253.43 | 22 | 12 |
(±)-19 | 17.92 | 108.69 | 209.01 | 6 | 12 |
(±)-20 | 24.4 | 170.52 | 285.54 | 7 | 12 |
(±)-21 | 0.61 | 262.74 | 32.03 | 431 | 52.5 |
(±)-22 | 0.53 | 118.34 | 44.85 | 223 | 85 |
(±)-23 | 0.25 | 95.18 | 44.11 | 380 | 176 |
(±)-24 | 0.74 | 61.19 | 40.42 | 83 | 55 |
(±)-25 | 0.87 | 78.75 | 27.35 | 90.5 | 31 |
(±)-26 | 0.74 | 108.55 | 58.72 | 147 | 79 |
(±)-27 | 0.66 | 201.61 | 83.9 | 305.5 | 127 |
(±)-28 | 0.414 | 63.22 | 23.76 | 153 | 57 |
(±)-29 | 0.483 | 76.13 | 44.23 | 158 | 92 |
(±)-30 | 0.589 | 16.47 | 20.46 | 28 | 35 |
(±)-31 | 1.891 | 58.14 | 75.36 | 31 | 40 |
(±)-32 | 0.088 | 123.90 | 18.17 | 1408 | 206.5 |
(±)-33 | 0.119 | 44.09 | 22.59 | 370.5 | 190 |
(±)-34 | 0.048 | 49.07 | 26.59 | 1022 | 554 |
The apparent Ki values are represented as the mean of two or more independent experiments preformed in duplicate with five or six data points each and correlation coefficients of 0.88–0.99. The experimental standard deviations were less than 10%.
n/e and n/i are the selectivity ratio of Ki (eNOS or iNOS) to Ki (nNOS).
L-NNA: L-Nω-nitroarginine, a positive control.