Table 1

Kd and B max values of [3H]diprenorphine binding to the wild-type, chimeric, and mutant κ opioid receptors stably expressed in CHO cells

Receptor ConstructKdBmaxn
nM pmol/mg of protein
hkor0.16  ± 0.021.22  ± 0.053
rkor0.20  ± 0.201.00  ± 0.143
Flag-hkor0.10  ± 0.021.33  ± 0.156
Flag-rkor0.26  ± 0.102.09  ± 0.316
Flag-r/hkor0.12  ± 0.012.74  ± 0.144
Flag-h/rkor0.10  ± 0.012.34  ± 0.133
Flag-rkorN358S0.13  ± 0.022.25  ± 0.033
Flag-hkorS358N0.08  ± 0.011.27  ± 0.156

Membranes were prepared from CHO cells stably expressing each receptor construct. Saturation binding of [3H]diprenorphine was performed and K d and B max values were determined. Results are expressed as mean ± S.E.M.n = number of independent experiments in duplicate.