Table 1. Inhibition of agonist-stimulated [35S]GTPγS binding in cloned human μ, δ, and κ opioid receptors.
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Compound | Ke (nM)a | μ/κ | δ/κ | ||
μ, DAMGO | δ, DPDPE | κ, U69,593 | |||
JDTic | 25 ± 4 | 74 ± 2 | 0.02 ± 0.01 | 1,250 | 3,800 |
1 | 3.96 ± 1.1 | 281 ± 44 | 0.051 ± 0.01 | 77 | 5,510 |
2 | 14.5 ± 2.6 | 590 ± 130 | 0.43 ± 0.12 | 33 | 1,372 |
3a | 45.4 ± 15 | 1140 ± 70 | 0.51 ± 0.08 | 89 | 2,235 |
3b | 49.2 ± 14 | >3000 | 0.18 ± 0.01 | 273 | >16,700 |
4a | 57.1 ± 15 | 690 ± 250 | 0.51 ± 0.14 | 112 | 1,353 |
4b | 154 ± 56 | 2,510 ± 490 | 1.75 ± 0.65 | 88 | 1,434 |
5 | 3.93 ± 0.73 | 118 ± 27 | 0.12 ± 0.02 | 33 | 983 |
Ke values are the mean ± SEM of at least three independent experiments performed in duplicates.