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. Author manuscript; available in PMC: 2017 Nov 23.
Published in final edited form as: J Med Chem. 2016 Nov 8;59(22):10291–10298. doi: 10.1021/acs.jmedchem.6b01411

Table 5.

Antagonist Mode [35S]GTPγS Assays of [des-Arg7]Dyn A Analogues at KOR

[35S]GTPγS bindinga
compd IC50 (nM)b Imax (%)c
naloxone 140 ± 58 100
1 NC NC
2 NC NC
3 NC NC
4 220 ± 28 110 ± 7
7 >2500 38d
14 750 ± 137 120 ± 4
16 >2500 29d
a

Expressed in KOR-CHO cells.

b

Concentration to afford 50% inhibition. Data reported as the mean ± SEM normalized to 100 nM U50,488 (100% stimulation).

c

Data are normalized to % of naloxone.

d

Percent inhibition at 10 µM; a full curve could not be fit.