In Vitro Binding Affinities and Functional Activities of LY2795050 at Cloned Human Opioid Receptors
| Ki (nM) | Antagonist activity (Kb, nM) | Agonist activity (EC50, nM) | |||||||
| Compound | κ | μ | δ | κ | μ | δ | κ | μ | δ |
| LY2795050 | 0.72 | 25.8 | 153 | 0.63 | 6.80 | 83.3 | >10,000 | >10,000 | >10,000 |
| Naltrexone | 1.88 | 0.62 | 12.3 | 2.26 | 0.47 | 11.3 | >10,000 | >10,000 | >10,000 |
| JDTic | 0.06 | 11.5 | 188 | 0.10 | 6.58 | 168 | >10,000 | >10,000 | >10,000 |
| GR103545 | 0.44 | 33.5 | 423 | >1,400 | 17.7 | >1,720 | 0.09 | >10,000 | 34.7 |
Data presented are mean of 3 separate determinations.