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Inhibition of Agonist-Stimulated [35S]GTPγS Binding in Cloned Human μ, δ, and κ Opioid Receptors for 12 and Three Isomers
 | |||||
|---|---|---|---|---|---|
| compd |
Ke (nM)a |
μ/κ | δ/κ | ||
| μ, DAMGO | δ, DPDPE | κ, U69,593 | |||
| 12 | 239 ± 22 | >3000 | 0.37 ± 0.09 | 645 | >8100 |
| 31 | 955 ± 280 | >3000 | 9.29 ± 3.2 | 103 | >323 |
| 32 | 479 ± 150 | >3000 | 11.5 ± 1.9 | 42 | >261 |
| 33 | >3000 | >3000 | 42.8 ± 4.0 | >70 | >70 |
Data are mean ± SEM of at least three independent experiments conducted in duplicate. None of the compounds had agonist activity at 10 μM.
