Table 2.
Inhibition of Agonist-Stimulated [35S]GTPγS Binding in Cloned Human μ, δ, and κ Opioid Receptors, Importance of Methyl Substituent of 1
 | |||||
|---|---|---|---|---|---|
| Compd |
Ke (nM)a |
μ/κ | δ/κ | ||
| μ,DAMGO | δ, DPDPE | κ, U69,593 | |||
| 1 | 144 ± 37 | >3000 | 6.80 ± 2.1 | 21 | >441 |
| 12 | 239 ± 22 | >3000 | 0.37 ± 0.09 | 646 | >8100 |
| 13b | 139 ± 1.0 | >3000 | 15.6 ± 2.3 | 9 | >192 |
| 14b | 44.9 ± 11 | >3000 | 15.1 ± 4.2 | 3 | >199 |
| 15b | 108 ± 26 | >3000 | 1.26 ± 0.08 | 86 | >2381 |
| 16b | 50.9 ± 7.7 | 2350 ± 390 | 2.3 ± 0.64 | 22 | 1022 |
| 17b | 30.3 ± 1.0 | >3000 | 3.46 ± 0.54 | 9 | >867 |
a
Data are mean ± SEM of at least three independent experiments conducted in duplicate. None of the compounds had agonist activity at 10 μM.
b
These compounds are mixtures of isomers.