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. 2012 Oct 8;55(22):9868–9874. doi: 10.1021/jm301096s

Table 2. Antagonist Activity (Ke, nM) for test Compounds at Opioid Receptors Determined in Mouse Vas Deferens.

  Ke, nMa
ligand MOR DOR KOR
3a 0.83 ± 0.04 6.84 ± 2.00 ND
6 0.20 ± 0.02 3.89 ± 0.99 1.05 ± 0.13
4a 0.72 ± 0.11 6.20 ± 3.28 1.89 ± 0.17
5a 0.021 ± 0.002 1.25 ± 0.38 0.047 ± 0.005
3bb 0.02 ± 0.007 0.25 ± 0.06 0.19 ± 0.06
4bc 0.56 ± 0.15 0.94 ± 0.14 1.24 ± 0.12
5bc 0.008 ± 0.0006 0.044 ± 0.005 0.052 ± 0.003
a

The selective agonists used were DAMGO (MOR), DPDPE (DOR), U69593 (KOR). ND = not determined. Buprenorphine is an agonist in the mouse vas deferens with an EC50 of 21 nM (ref (14)).

b

Data from ref (21).

c

Data from ref (6).