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Opioid receptor binding affinities for U-47700 and its N-desmethyl metabolites in post-mortem rat brain tissue.
| Compound | μ-opioid receptor Ki (nM) | δ-opioid receptor Ki (nM) | κ-opioid receptor Ki (nM) | μ/δ ratio | μ/κ ratio |
|---|---|---|---|---|---|
| U-47700 | 11.1±0.4 | 1220±82 | 287±24 | 110 | 26 |
| N-Desmethyl-U-47700 | 206±11 | >10,000 | 1730±196 | >49 | 8 |
| N,N-Didesmethyl-U-47700 | 4080±304 | >10000 | 6770±814 | >2 | >2 |
| Morphine | 2.7±0.3 | 261±24 | 101±9 | 97 | 37 |
Data are expressed as mean±SEM for N=3 experiments performed in triplicate.
