Effects of tachykinin receptor ligands on125I-[MePhe7]-NKB binding and Ca2+mobilization in (hNK-4R) and hNK-3R cells
| Binding (Inhibition of125I-[MePhe7]-NKB) | Ca2+Mobilization | |||
|---|---|---|---|---|
| hNK-4R IC50 | hNK-3R IC50 | hNK-4R EC50 | hNK-3R EC50 | |
| nM | ||||
| Agonists | ||||
| NKB | 18.3 ± 3.3 | 8.9 ± 0.2 | 0.2 ± 0.1 | 0.3 ± 0.2 |
| [MePhe7]-NKB | 3.3 ± 0.5 | 1.8 ± 1.0 | 0.4 ± 0.2 | 0.3 ± 0.1 |
| Senktide | 15.1 ± 2.6 | 55 ± 19 | 0.3 ± 0.1 | 0.1 ± 0.03 |
| NKA | 3,530 ± 180 | 3,300 ± 240 | 18 ± 11 | 22 ± 4 |
| Substance P | 2,130 ± 540 | 7,660 ± 3,090 | 39 ± 16 | 97 ± 16 |
| Inhibition of NKB (1 nM) IC50 | Inhibition of NKB (1 nM) IC50 | |||
|---|---|---|---|---|
| nM | ||||
| Antagonists | ||||
| SB 223412 | 4.1 ± 0.7 | 1.1 ± 0.1 | 50 ± 34 | 125 ± 46 |
| SR 142801 | 2.6 ± 0.6 | 3.8 ± 0.3 | 254 ± 180 | 231 ± 110 |
| SR 222200 | 11.0 ± 2.7 | 18.1 ± 5.4 | 108 ± 52 | 264 ± 73 |
| SR 48968 | 711 ± 120 | 1,250 ± 160 | 1,212 ± 660 | 14,600 (2) |
| CP 99994 | 8,500 ± 2,400 | 23,000 ± 4,100 | >100,000 (2) | >10,000 (2) |
The experimental protocols for these studies are given underExperimental Procedures. Results are presented as EC50 or IC50 values and are the mean ± S.E. or the mean; n = 3 unless indicated in parentheses.