Table 1. Competitive inhibition experiments of [3H]RX821002 versus NE, DA, clonidine and D2-like receptor ligands in sheep brain cortex and striatum.
LIGAND | BINDING PARAMETERS | |
---|---|---|
| ||
CORTEX | STRIATUM | |
KDB1: 0.3 ± 0.2 * | KDB1: 0.8 ± 0,1 | |
NE | KDB2: 250 ± 100 | KDB2: 5000 ± 3000 |
DCB: -2.3 | DCB: -3.2 | |
| ||
KDB1: 6.9 ± 0.2 | KDB1: 6 ± 1 | |
DA | KDB2: 350 ± 10 * | KDB2: 1000 ± 200 |
DCB: -1.1 | DCB: -1.6 | |
| ||
KDB1: 0.014 ± 0.003 * | KDB1: 0.036 ± 0.005 | |
Clonidine | KDB2: 40 ± 20 | KDB2: 20 ± 10 |
DCB: -2.8 | DCB: -2.1 | |
| ||
KDB1: 9 ± 2 ** | KDB1: 51 ± 6 | |
7-OH-PIPAT | KDB2: 430 ± 80 | |
DCB: -1.1 | DCB: 0 | |
| ||
KDB1: 530 ± 50 ** | KDB1: 110 ± 10 | |
Quinpirole | KDB2: 2700 ± 400 | |
DCB: 0 | DCB: -0.8 | |
| ||
KDB1: 0.055 ± 0.003 *** | KDB1: 0.42 ± 0.03 | |
RO-105824 | KDB2: 4000 ± 2000 | |
DCB: -4.3 | DCB: 0 |
Binding parameters from competitive-inhibition experiments of [3H]RX821002 versus NE, DA, clonidine and D2-like receptor ligands in membrane preparations from sheep brain cortex and striatum (Fig. 2). KDB1, KDB2 and DCB values were obtained according to the two-state dimer model (see Materials and Methods and ref. 22). KDB1 and KDB2 (in nM) are expressed as means ± S.E.M. of 3 experiments performed in triplicate. Statistical differences between affinity parameters of cortical versus striatal adrenoceptors were calculated by non-paired, two-tailed Student's t test;
p<0.05,
p<0.01 and
p<0.001.