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Potency and selectivity of GW274150 compared with GW273629 and L-NMMA on iNOS vs eNOS and nNOS in intact rat tissue assays
| Compound | Vascular ring NO synthesis ED50 (μM) (selectivity for iNOS) | Brain slice NO synthesis IC50 (μM) (selectivity for iNOS) | |
|---|---|---|---|
| iNOS | eNOS | nNOS | |
| GW274150 | 1.15±0.56 | 43% inhibition at 300 μM (>260) | 252±1.1 (219) |
| GW273629 | 2.0±0.6 | 45% inhibition at 300 μM (>150) | 729±181 (365) |
| L-NMMA | 5.2±0.8 | 16.3±1.5 (3.1) | 12.6±0.5 (2.4) |
Fold selectivities for iNOS are shown in brackets.
