Table 2.

[³⁵S]GTP-γ-S functional assay for compounds 3, 4, 5, 7,8a, and 14.

Cmpd	ED50 ± SDa (κ) nM	Emax ± SDb (κ)
1c	40 ±10	120 ± 2
3	6 ± 1	118 ± 2
4	0.65 ± 0.17	127 ± 5
5	60 ± 6	109 ± 3
7a	1220 ± 230	112 ± 8
7b	690 ± 80	103 ± 4
8a	150 ± 14	101 ± 3
14	1934 ± 239	113 ± 5

^aED₅₀ = Effective dose for 50% maximal response.

^bEmax is % at which compound stimulates [³⁵S]GTP-γ-Sbinding compared to (−)-U50,488 (500 nM) at KOP receptors.

^cData from reference 21.