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. Author manuscript; available in PMC: 2014 Mar 28.
Published in final edited form as: J Med Chem. 2013 Feb 14;56(6):2178–2195. doi: 10.1021/jm301783x

Table 2.

Inhibition of Agonist Stimulated [35S]GTPγS Binding by Compounds in Cloned Human MOR, DOR, and KOR

graphic file with name nihms442171u2.jpg
Compd Ke (nM)
μ/κ δ/κ
DAMGO, μ DPDPE, δ U69,593, κ
2 (nor-BNI 26 29 0.05 520 580
3 (JDTic) 25 76 0.02 1250 3800
24a (KAA1) 42 33 0.24 175 138
24b 176 313 0.47 374 666
24c 259 77 2.2 118 35
24d 82 186 0.87 94 214
24e 48 13 0.09 533 144
24f 26 32 0.30 87 107
24g 52 62 0.09 578 689
24h 4.6 25 0.07 66 357
24i 28 25 0.04 700 625