Table 1

Summary of the radio-ligand binding and electrophysiology assay data for human members of opioid receptor gene family

Expression LevelDiprenorphineNociceptinDynorphin A
Bmax (fmol/mg protein)Kd(nM)Kd (nM)Ki(nM)EC50 (nM)
hMOR4364  ± 2162.9  ± 0.71.60  ± 0.1830  ± 5
hDOR4901  ± 1861.8  ± 0.41.25  ± 0.1284  ± 11
hKOR1262  ± 440.8  ± 0.50.05  ± 0.010.43  ± 0.08
hORL1739  ± 380.81  ± 0.12386  ± 4730  ± 6
  • [3H]-diprenorphine was used as radiolabeled ligand in hMOR, hDOR and hKOR binding, [3H]-nociceptin was used in hORL1 binding. The Ki values were calculated according to the Cheng-Prusoff equation from the binding studies. EC50 values were obtained from electrophysiology studies.