Demonstration of the heterogeneity of the kappa-opioid receptors in guinea-pig cerebellum using selective and nonselective drugs.

@article{Tiberi1990DemonstrationOT,
  title={Demonstration of the heterogeneity of the kappa-opioid receptors in guinea-pig cerebellum using selective and nonselective drugs.},
  author={Monica Tiberi and Jacques Magnan},
  journal={European journal of pharmacology},
  year={1990},
  volume={188 6},
  pages={379-89}
}
In guinea-pig cerebellum, saturation studies reveal that the nonselective opioid [3H]ethylketazocine has a binding capacity (R) of 6.79 pmol/g tissue which is similar to the sum of the individual R values of the mu-, delta- and kappa 1-selective opioids. Conversely, the binding parameters of the nonselective opioid [3H]bremazocine are best-fitted to a two-site model (Kd1 = 0.12 nM, R1 = 11.3 pmol/g tissue; Kd2 = 6.03 nM, R2 = 9.09 pmol/g tissue) with an R TOTAL value of 20.3 pmol/g tissue which… CONTINUE READING