Table 3.
Comparison of type-selectivity of opioid ligands for hMOR in present study with previously reported type-selectivities for hMOR in Toll et al. 1998 study. The degree of type-selectivity was determined by calculating the ratios of opioid Ki values for delta- vs. mu-selective and kappa- vs. mu-selective ligands.
| Type-Selective Opioids | Present Studya | Toll et al. 1998b | ||
|---|---|---|---|---|
| Ki (nM) | Ratio | Ki (nM) | Ratio | |
| Agonists | ||||
| DPDPE/DAMGO (delta/mu) | 11,690/268 | 44 | 504/0.5 | 1,008 |
| U-50,488/DAMGO (kappa/mu) | 5,561/268 | 21 | 290/0.5 | 580 |
| Antagonists | ||||
| NTI/β-FNA (delta/mu) | 6.10/1.85 | 3.2 | 6.3/0.3 | 21 |
| Nor-BNI/β-FNA (kappa/mu) | 67.4/1.85 | 35 | 21/0.3 | 70 |
Opioid ligand binding was conducted in intact cells in Hank's balanced salts buffer at pH 7.4
Opioid ligand binding was conducted using cell membrane homogenates in 50mM Tris-HCl pH 7.5.