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. Author manuscript; available in PMC: 2012 Oct 13.
Published in final edited form as: J Med Chem. 2011 Sep 7;54(19):6531–6537. doi: 10.1021/jm2003238

Table 1.

Binding affinities to opioid and NOP receptors.

Ki (nM) ± SEMa
NOP MU DELTA KAPPA
Nociceptin 0.08 ± 0.03 437 ± 13 2846 ± 512 147 ± 3.4
DAMGO > 10,000 1.59 ± 0.17 300 ± 59 306 ± 46
DPDPE > 10,000 504 ± 10 1.24 ± 0.09 > 10,000
U69,593 > 10,000 > 10,000 > 10,000 1.6 ± 0.26
1a 77.4 ± 16 1.5 ± 0.8 6.1 ± 0.4 2.5 ± 1.2
1b 8.46 ± 1.3 2.14 ± 0.79 1.59 ± 0.28 5.63 ± 1.3
1c 18.5 ± 0.68 2.95 ± 0.65 1.27 ± 0.21 1.59 ± 0.25
1d 22.0 ± 0.55 2.19 ± 0.65 3.66 ± 0.92 4.15 ± 1.3
1e 133 ± 8.2 5.56 ± 1.3 3.03 ± 0.61 8.92 ± 0.34
1f 16.0 ± 1.5 11.4 ± 0.17 7.13 ± 1.3 9.87 ± 1.3
6a 237 ± 64 14.3 ± 0.88 6.79 ± 0.99 9.93 ± 3.7
6b 67.8 ± 20 13.2 ± 0.97 17.2 ± 0.26 45.6 ± 3.4
7 159 ± 1.4 10.5 ± 3.86 8.67 ± 0.81 35.5 ± 3.9
a

Binding to cloned human opioid receptors transfected into CHO cells (method in ref 25). Values are the average of two experiments each carried out in duplicate. Tritiated ligands were [3H]DAMGO (MOP), [3H]Cl-DPDPE (DOP), [3H]U69593 (KOP) and [3H] N/OFQ