Table 1.
Summary of the pharmacological profile of nonpeptide NOP agonists in comparison with N/OFQ
| GTPγ[35S] | Calcium mobilization | Bioluminescence resonance energy transfer | Mouse Vas Deferens | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| G protein | β‐arrestin 2 | ||||||||||||
| CR | α | CR | α | Selectivity (NOP vs OP) | CR | α | CR | α | Bias factor | CR | α | Selectivity(+/+ vs. −/−) | |
| N/OFQ | 1 | 1.00 | 1 | 1.00 | >10000 | 1 | 1.00 | 1 | 1.00 | 0.00 | 1 | 1.00 | >100 |
| Ro 65‐6570 | 12 | 1.11 | 14 | 0.98 | 270 | 16 | 0.96 | 65 | 0.74 | 1.64 | 4 | >1 | 7 |
| Ro 2q | 14 | 0.88 | 10 | 0.99 | 100 | 28 | 0.93 | 63 | 0.43 | 0.93 | 1.70 | >1 | 3 |
| SCH‐221510 | 13 | 1.04 | 36 | 0.94 | 60 | 36 | 1.10 | 55 | 0.84 | 1.10 | 11 | >1 | 2 |
| MCOPPB | 0.30 | 1.19 | 0.52 | 1.03 | 1500 | 0.53 | 1.04 | 1 | 0.99 | 0.97 | 0.71 | >1 | 14 |
| AT‐403 | 1.20 | 0.91 | 1 | 0.96 | 1500 | 4 | 0.94 | 5 | 0.79 | 0.16 | 0.40 | >1 | 30 |
| AT‐202 | 48 | 0.95 | 120 | 1.01 | 250 | 90 | 0.96 | 105 | 0.89 | 0.46 | 6 | >1 | 9 |
| SCH‐486757 | 155 | 1.12 | 380 | 0.99 | 80 | 135 | 0.82 | 178 | 0.36 | 0.81 | ‐ | ||
Agonist efficacy is expressed as intrinsic activity (α) calculated as the ratio between the E max of the ligand and that of the standard agonist N/OFQ.
Agonist potency is expressed as concentration ratio (CR) calculated as the ratio between the EC50 of the ligand and that of the standard agonist N/OFQ.