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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 1.

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

graphic file with name nihms442171u1.jpg
Compd R1 R2 R3 R4 R5 Ke (nM)
μ/κ δ/κ
DAMGO, μ DPDPE, δ U69,593, κ
2 (nor-BNI) 26 29 0.05 520 580
3 (JDTic) H OH H H H 3.41 79.3 0.01 341 7930
23a CH3 OH H H H 51 118 0.06 850 1966
23b H OCH3 H H H 24 21.2 0.037 649 573
23c H OH CH3 H H 3 24 0.03 100 800
23d H OH H CH3 H 3.6 854 0.03 120 28500
23e H OH H H CH3 210 491 0.16 1313 3070
23f H CONH2 H H H 21 480 0.12 175 400