Table 6.
Inhibition of Agonist-Stimulated [35S]GTPγS Binding in Cloned Human μ, δ, and κ Opioid Receptors, Importance of the Isopropyl and 7-Hydroxy-d-Tic Groups
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---|---|---|---|---|---|
compd |
Ke (nM)a |
μ/κ | δ/κ | ||
μ, DAMGO | δ, DPDPE | κ, U69,593 | |||
34 | >3000 | >3000 | 113 ± 21 | >27 | >27 |
35 | 586 ± 130 | >3000 | 5.58 ± 1.6 | 105 | >538 |
36 | >3000 | >3000 | 387 ± 89 | >8 | >8 |
37 | 431 ± 110 | >3000 | 20.5 ± 4.6 | 21 | >146 |
38 | 153 ± 37 | >3000 | 11.1 ± 2.9 | 14 | >270 |
39 | 569 ± 110 | >3000 | 17.2 ± 5.8 | 33 | >174 |
Data are mean ± SEM of at least three independent experiments conducted in duplicate. None of the compounds had agonist activity at 10 μM.