Affinities of opiate alkaloid and opioid peptide agonists and antagonists for wild-type, H297N, and H297Q μ receptors
| Wild-type | H297N | H297Q | |
|---|---|---|---|
| Kd n m | |||
| Naloxone | 1.2 ± 0.1 | 6.7 ± 0.1 | 2.0 ± 0.6 |
| Kin m | |||
| DAMGO | 2.7 ± 0.3 | 5.8 ± 0.5 | 2.9 ± 0.6 |
| PL017 | 38.3 ± 0.5 | 42.9 ± 5.2 | 7.9 ± 0.6 |
| Morphine | 35.8 ± 3.0 | 46.7 ± 8.0 | 24.4 ± 3.9 |
| Sufentanyl | 1.3 ± 0.3 | 0.8 ± 0.1 | 1.1 ± 0.3 |
| Buprenorphine | 1.6 ± 0.3 | 2.2 ± 0.4 | 2.1 ± 0.4 |
| CTOP | 3.7 ± 0.3 | 9.9 ± 2.5 | 2.0 ± 0.4 |
Values are mean ± standard error from at least four experiments.