Extended Data Table 4 |.
Efficacy table for drugs profiled in Extended Data Fig. 6
| Efficacy | ||||||||
|---|---|---|---|---|---|---|---|---|
|
| ||||||||
| Compounds | Gi1 Emax % ± SEM |
Gi2 Emax % ± SEM |
Gi3 Emax % ± SEM |
G0a Emax % ± SEM |
G0b Emax % ± SEM |
Gz Emax % ± SEM |
β-arrl Emax % ± SEM |
β-arr2 Emax % ± SEM |
| Opioid Peptides | ||||||||
| DAMGO | 99 ± 2 | 98 ± 3 | 98 ± 2 | 99 ± 2 | 100 ± 2 | 100 ± 2 | 100 ± 3.1 | 99± 2.8 |
| Endomorphin-1 | 93 ± 1.6 | 95 ± 1.7 | 96 ± 1.4 | 109 ± 2.7 | 91 ± 2.6 | 105 ± 1.1 | 78 ± 3.1 | 82 ± 2.5 |
| Leu-Enkephalin | 92 ± 5.5 | 85 ± 7.2 | 93 ± 4.7 | 96 ± 3.8 | 102 ± 4.5 | 103 ± 5.2 | 100 ± 6.2 | 97 ± 6.8 |
| Met-Enkephalin | 92 ± 4.6 | 84 ± 6.6 | 103 ± 5.6 | 97 ± 3.7 | 96 ± 3.1 | 96 ± 3.1 | 102 ± 4.9 | 92 ± 4.5 |
| Beta-Enkephalin | 87 ± 3.6 | 102 ± 6.1 | 99 ± 2.8 | 91 ± 3.2 | 99 ± 5.9 | 104 ± 4.5 | 76 ± 4.8 | 90 ± 5.3 |
| Dynorphin 1–17 | 92 ± 2.3 | 86 ± 3.8 | 90 ± 2.4 | 94 ± 4.4 | 92 ± 3.0 | 103 ± 1.4 | 50 ± 15 | 42±1.03 |
|
| ||||||||
| Biased Opiates | ||||||||
| PZM21 | 72 ± 2.0 | 84 ± 3.0 | 68 ± 1.9 | 92 ± 4.0 | 84 ± 3.1 | 98 ± 1.6 | 38 ± 3.3 | 24 ± 3.7 |
| 7-OH | 31 ± 4.9 | 53 ± 5.1 | nd | 65 ± 4.9 | 56 ± 3.5 | 73 ± 2.8 | nd | nd |
| TRV130 | 58 ± 3.8 | 58 ± 4.2 | 45 ± 3.3 | 67 ± 5.3 | 76 ± 4.4 | 98 ± 2.2 | nd | 26 ± 5.9 |
|
| ||||||||
| Partial agonists | ||||||||
| Pentazocine | 75 ± 1.8 | 78 ± 3.8 | 73 ± 2.3 | 89 ± 4.0 | 89 ± 3.2 | 103 ± 1.5 | 7±4.51 | 13±4.04 |
| Buprenorphine | 59 ± 3.6 | 60 ± 3.7 | 38 ± 4.0 | 70 ± 4.3 | 68 ± 3.3 | 77 ± 3.5 | nd | nd |
|
| ||||||||
| Prototypic agonists | ||||||||
| Oxycodone | 82 ± 3.2 | 83 ± 5.7 | 75 ± 3.8 | 102 ± 5.2 | 110 ± 3.4 | 102 ± 4.9 | 81 ± 7.9 | 80 ± 3.9 |
| Carfentanil | 97 ± 1.8 | 99 ± 2.2 | 102 ± 1.8 | 119 ± 3.8 | 96 ± 4.1 | 112 ± 1.7 | 96 ± 7.0 | 97 ± 6.7 |
| Fentanyl | 105 ± 4.8 | 89 ± 6.2 | 92 ± 6.5 | 91 ± 4.3 | 100 ± 4.2 | 90 ± 3.4 | 92 ± 2.2 | 97 ± 3.4 |
| Morphine | 99 ± 4.1 | 86 ± 5.5 | 79 ± 6.2 | 93 ± 3.9 | 96 ± 3.2 | 98 ± 4.6 | 29 ± 2.0 | 37 ± 4.2 |
|
| ||||||||
| Bitopics | ||||||||
| C3-guano | 71 ± 6.3 | 90 ± 6.5 | 70 ± 8.5 | 78 ± 5.1 | 83 ± 3.6 | 82 ± 5.3 | n.d. | 37 ± 11 |
| C5-guano | 80 ± 3.6 | 90 ± 3.7 | 85 ± 5.5 | 92 ± 2.3 | 87 ± 3.7 | 86 ± 3.2 | 32 ± 3.0 | 38 ± 5.3 |
| C6-guano | 71 ± 7.7 | 79 ± 7.2 | 56 ± 6.1 | 52 ± 7.0 | 64 ± 4.1 | 50 ± 5.3 | n.d. | 23±7.6 |
| C7-guano | 26 ± 1.8 | 38 ± 2.6 | 31 ± 5.2 | 45 ± 2.7 | 38 ± 2.6 | 73 ± 2.8 | n.d. | n.d. |
| C9-guano | 83 ± 3.4 | 96 ± 5.5 | 98 ± 4.6 | 95 ± 4.0 | 96 ± 2.8 | 99 ± 4.2 | 29 ± 2.7 | 61 ± 7.0 |
| C11-guano | 41 ± 2.5 | 45 ± 3.7 | 43 ± 5.2 | 54 ± 3.4 | 67 ± 3.2 | 82 ± 3.2 | n.d. | 80 ± 12 |
Efficacy (Emax% ± SEM) are reported as estimates from simultaneous curve fitting of all biological replicates and include standard error.