TABLE 1

Saturation ligand binding analyses for [3H]nemonapride, [3H]raclopride, and [3H]spiperone binding to D2 dopamine receptors expressed in Sf9 cells Saturation binding studies were performed as described under Materials and Methods section with [3H]nemonapride, [3H]raclopride, and [3H]spiperone using different preparations of Sf9 cell membranes expressing the D2 dopamine receptor, under control conditions or with 100 mM sodium ions. Experiments with preparation 3 included 0.1% bovine serum albumin as described under Materials and Methods. All saturation analyses fitted best to one-binding site models from which Bmax (pmol/mg) and pKd values were determined and are expressed as mean ± S.E.M. from three or more experiments.

Radioligand Bmax pKd
Preparation 1 Preparation 2 Preparation 3 Preparation 1 Preparation 2 Preparation 3
Control Na+ Control Na+ Control Na+ Control Na+ Control Na+ Control Na+
[3H]Nemonapride 0.92 ± 0.04 1.53 ± 0.04* 4.13 ± 0.17 5.28 ± 0.26* 3.37 ± 0.26 6.13 ± 0.28* 9.81 ± 0.20 10.76 ± 0.11* 10.02 ± 0.03 10.34 ± 0.12* 9.62 ± 0.07 10.51 ± 0.06*
[3H]Raclopride N.D. 0.32 ± 0.18 N.D. 2.32 ± 0.29 N.D. 2.20 ± 0.60 N.D. 8.67 ± 0.15 N.D. 8.69 ± 0.05 N.D. 8.83 ± 0.11
[3H]Spiperone 0.98 ± 0.06 0.99 ± 0.06 4.03 ± 0.75 4.23 ± 0.23 2.64 ± 0.19 3.54 ± 0.15* 10.47 ± 0.06 10.35 ± 0.06 10.01 ± 0.09 9.77 ± 0.13 9.99 ± 0.07 9.81 ± 0.03*
  • N.D., not determined because no saturable high-affinity binding could be detected.

  • * Different from control (P < 0.05)