Selectivity profile of [D-Cys(tBu)5]NPS at seven different G-protein-coupled receptors Data are mean ± S.E.M. of three separate experiments performed in duplicate. The chimeric protein αqi5 (Coward et al., 1999) was used to force opioid receptors to couple with the calcium pathway.
Cell Lines | Receptor | Agonist | Control | [D-Cys(tBu)5]NPS (10 μM) | ||||
|---|---|---|---|---|---|---|---|---|
| pEC50 | Emax ± S.E.M. | pEC50 | Emax ± S.E.M. | |||||
| % above baseline | % above baseline | |||||||
| HEK293 | Native muscarinic | Carbachol | 5.60 (5.21–5.69) | 309 ± 31 | 5.44 (4.82–6.06) | 309 ± 33 | ||
| CHO | Recombinant hNK-1 | Substance P | 10.26 (9.88–10.64) | 122 ± 15 | 10.10 (9.51–10.69) | 110 ± 20 | ||
| CHO | Recombinant hUT | Urotensin-II | 8.31 (7.62–9.00) | 224 ± 21 | 8.37 (7.54–9.20) | 225 ± 23 | ||
| CHO-αqi5 | Recombinant hMOP | Dermorphin | 7.98 (7.85–8.11) | 186 ± 11 | 7.80 (7.16–8.44) | 194 ± 13 | ||
| CHO-αqi5 | Recombinant hDOP | [D-Pen2,D-Pen5]-enkephalin | 8.63 (8.41–8.84) | 169 ± 26 | 8.65 (8.52–8.78) | 155 ± 22 | ||
| CHO-αqi5 | Recombinant hKOP | Dynorphin A | 8.11 (7.72–8.50) | 143 ± 12 | 8.53 (8.00–9.06) | 144 ± 12 | ||
| A549 | Native hPAR-2 | SLIGKV-NH2 | 4.66 (4.43–4.89) | 449 ± 25 | 4.77 (4.31–5.23) | 433 ± 37 | ||