Table 2. Competitive inhibition experiments of [3H]SCH 23390, [3H]YM-09151-2 or [3H]RX821002 versus DA and NE in sheep brain striatum.
RECEPTOR | BINDING PARAMETERS | |
---|---|---|
| ||
DA | NE | |
KDB1: 8 ± 3 | KDB1: 53 ± 90## | |
D1-like | KDB2: 8000 ±1000*** | KDB2: 50000 ± 10000# |
Dc: -2.4 | Dc: -2.4 | |
| ||
KDB1: 3.5 ± 0.6 | KDB1: 60 ± 40## | |
D2-like | KDB2: 700 ± 200 | KDB2: 3400 ± 100 |
Dc: -1.7 | Dc: -1.2 | |
| ||
KDB1: 6 ± 1 | KDB1: 0.8 ± 0.1 | |
α2 | KDB2: 1000 ± 200 | KDB2: 5000 ± 3000 |
Dc: -1.6 | Dc: -3.2 |
Binding parameters from competitive-inhibition experiments of [3H]SCH 23390 (D1-like receptor antagonist), [3H]YM-09151-2 (D2-like receptor antagonist) or [3H]RX821002 (α2 receptor antagonist), versus NE and DA in sheep brain striatum. KDB1, KDB2 and Dc values were obtained according to the two-state dimer model (see Materials and Methods and ref. 22). Values for α2- adrenoceptors are from Table 1. KDB1 and KDB2 (in nM) are expressed as means ± S.E.M. of 3-5 experiments performed in triplicate. Statistical differences between affinity parameters obtained were calculated by one-way ANOVA followed by Dunnett's post hoc test; for DA,
p<0.001 vs. D2-like receptors; for NE,
p<0.05 and
p<0.01 vs. α2 receptors.