. Author manuscript; available in PMC: 2014 Nov 14.

Published in final edited form as: J Med Chem. 2013 Oct 29;56(21):10.1021/jm401290y. doi: 10.1021/jm401290y

TABLE 2.

Stimulation/Inhibition of [³⁵S]GTPγS Binding Mediated by the MOR and KOR.

Compound	MOR				KOR
Compound	E_max (%)	EC₅₀ (nM)	I_max (%)	IC₅₀ (nM)	E_max (%)	EC₅₀ (nM)	I_max (%)	IC₅₀ (nM)
1a^b	45 ± 4	73 ± 5	NI	NA	80 ± 6	2.4 ± 0.6	NI	NA
1b^c	40 ± 0.87	47 ±9.0	NI	NA	82 ± 10	14 ± 3.1	NI	NA
1c^c	83 ± 2.5	29 ± 4.6	NI	NA	190 ± 6.4	22 ± 5.1	NI	NA
7^d	24 ± 0.90	39 ±7.8	69 ± 2.4	640 ± 76	140 ± 4.9	49 ± 1.3	NI	NA
8^d	34± 2.3	0.41 ± 0.021	64 ± 3.6	3.0 ± 0.56	59 ± 2.5	0.61 ± 0.049	49 ± 3.7	1.8 ± 0.20
9	34 ± 2.6	0.52 ± 0.086	70 ± 2.1	1.8 ± 0.38	72 ± 4.2	3.3 ± 0.27	44 ± 0.25	12 ± 1.4
10	47 ± 3.6	80 ± 13	60 ±0.55	500 ± 58	120 ± 2.4	140 ± 6.7	NI	NA
11	28 ± 1.7	51 ± 6.6	76 ± 0.68	650 ± 100	140 ± 5.8	97 ± 6.9	NI	NA
12	25 ± 1.7	0.52 ±0.076	76 ± 2.3	2.5 ± 0.26	85 ± 10.0	1.3 ± 0.10	27 ± 2.7	2.8 ± 0.42

Membranes from CHO cells that stably expressed the human MOR were incubated with varying concentrations of the compounds in the presence of 0.08 nM [³⁵S]GTPγS. Data are the mean values ± SEMs from three experiments, performed in triplicate. NI= No Inhibition NA=Not Applicable.

Ref. 18.

Ref. 19.