CysLT1 antagonists: effects in human lung preparations
| Tissue | Agonists | MK 571 | ICI 198,615 | BAYu9773 |
|---|---|---|---|---|
| Contraction | ||||
| Bronchus | LTC4 | 8.6–8.3 | 9.8–8.5 | 5.4 |
| LTD4 | 8.8–8.5 | 9.2–8.2 | 6.8–6.2 | |
| Pulmonary artery | LTC4 | NS | NS | NS |
| (7.20) | (7.02) | (6.26) | ||
| LTD4 | NS | NS | NS | |
| (NS) | (NS) | (NS) | ||
| Pulmonary vein | LTC4 | NS | NS | 6.7–5.8 |
| LTD4 | NS | NS | 6.8–6.5 | |
| Relaxation | ||||
| Pulmonary artery | LTD4 | NS | NS | ND |
| Pulmonary vein | LTD4 | NS | NS | ND |
The range of pK B values are shown. NS indicates no significant displacement of the concentration effect curves. ND indicates no data available. Numbers in parentheses are the pK B values derived from tissues (Walch et al., 2002) where the endothelium had been removed and the preparations treated with indomethacin. The other values are from references: Hay et al., 1987; Jones et al., 1989; Buckner et al., 1990; Labat et al., 1992; Ortiz et al., 1995; Gorenne et al., 1996; Bäck et al., 2000b.