Table 1. Receptor expression levels and ligand binding affinities of the hKOR-WT and hKOR-10KR.
Membranes of CHO cells stably expressing the FLAG-hKOR or FLAG-hKOR-10KR were prepared and Bmax and Kd values of [3H]diprenorphine and Ki values of U50,488H and Dyn A were determined as described in Materials and Methods. Each value represents the mean ± s.e.m. of three independent experiments.
| [3H]diprenorphine | U50,488H | Dyn A | ||
|---|---|---|---|---|
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| Bmax (pmol/mg protein) | Kd (nM) | Ki (nM) | Ki (nM) | |
| hKOR-WT | 1.71 ± 0.17 | 0.12 ± 0.01 | 1.45 ± 0.14 | 0.10 ± 0.01 |
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| HKOR-10KR | 2.20 ± 0.17 | 0.14 ± 0.02 | 1.64 ± 0.26 | 0.11 ± 0.02 |