TABLE 1

Competition binding data for [3H]N-methylspiperone sites at TM5 serine mutants

Values represent mean ± S.E.M. The expression of these receptors was as follows: WT: KD, 0.58 nM; Bmax, 4.8 pmol/mg; S5.42A: KD, 0.59 nM; Bmax, 4.0 pmol/mg; S5.43A: KD, 1.4 nM; Bmax, 20.7 pmol/mg; S5.46A: KD, 0.50 nM; Bmax, 2.3 pmol/mg.

MutantK0.5
WTS5.42AS5.43AS5.46A
nM
DNS144 ± 17660 ± 190750 ± 370330 ± 160
DNX83 ± 52700 ± 990*770 ± 90580 ± 340
DHX490 ± 917400 ± 1000*2,600 ± 501600 ± 40
Quinpirole365 ± 61040 ± 10027,000 ± 10,000*2900 ± 820
Dopamine450 ± 17080,000 ± 3000*31,000 ± 6000*3500 ± 1,500
  • * Significantly different from WT (P < 0.05; one-way ANOVA and Tukey-Kramer Multiple Comparisons Test).