Table 2. Agonist potencies (pEC50) and intrinsic activity (α), and antagonist potencies (pKB) of the compounds tested in the CHONOP cell DMR assay.
| pEC50 | α | pKB | |
|---|---|---|---|
| N/OFQ | 8.33 (7.63–9.04) |
1.00 | |
| N/OFQ(1–13)NH2 | 8.80 (8.07–9.53) |
1.30 | |
| [Arg14,Lys15]N/OFQ | 8.63 (7.48–9.77) |
1.32 | |
| UFP-112 | 8.66 (7.47–9.84) |
1.21 | |
| PWT2-N/OFQ | ~8.00 | 0.97 | |
| [Nphe1]N/OFQ(1–13)NH2 | 6.88 (5.80–7.96) |
0.88 | |
| [F/G]N/OFQ(1–13)NH2 | 8.06 (7.48–8.64) |
0.98 | |
| Ac-RYYRIK-NH2 | 9.30 (8.49–10.12) |
0.89 | |
| Ro 65–6570 | ~7.30 | 1.02 | |
| AT-090 | 8.40 (7.46–9.34) |
1.23 | |
| AT-127 | 7.97 (7.42–8.17) |
0.93 | |
| UFP-101 | crc incomplete | 7.60 (7.44–7.76) |
|
| SB-612111 | inactive | 8.25 (7.98–8.53) |
|
| J-113397 | inactive | 7.65 (7.45–7.85) |
|
| C-35 | inactive | 8.07 (7.90–8.24) |
|
| C-24 | inactive | 8.30 (8.04–8.57) |
|
Inactive means that up to 1 μM the compound did not promote any DMR response.