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Table 2 Agonist activities at the MOP receptor

From: Exploring pharmacological activities and signaling of morphinans substituted in position 6 as potent agonists interacting with the μ opioid receptor

  [ 35S]GTPγS functional assay a Calcium mobilization assay b
  EC 50(nM) E max(%) c EC 50(nM) E max(%) c
Oxycodone 500 ± 128 92 ± 9 1,176 ± 347 38 ± 3
14-OMC 325 ± 94 137 ± 55 973 ± 204 72 ± 7
1 273 ± 24 98 ± 4 957 ± 233 57 ± 4
2 42.5 ± 14.9 97 ± 15 116 ± 9 69 ± 7
3 26.2 ± 1.7 85 ± 3 140 ± 21 61 ± 6
4 25.6 ± 9.5 107 ± 26 56.1 ± 11.3 59 ± 8
5 1.64 ± 0.19 133 ± 7 21.7 ± 5.5 70 ± 8
6 25.1 ± 3.6 121 ± 27 173 ± 21 84 ± 10
DAMGO 20.2 ± 5.6 100 42.7 ± 7.6 100
  1. aMembranes from CHO cells stably transfected with human MOP receptors were used. bCHO cells co-expressing Gαqi5 protein and recombinant human MOP receptor were used. cEmax is expressed in percentage relative to maximal DAMGO induced stimulation in each assay (225 ± 32% and 217 ± 21% in [35S]GTPγS functional and calcium mobilization assay, respectively, set as 100%). Values represent the mean ± SEM of at least three experiments each performed in duplicate or triplicate.