Table 2. Properties of Agonist and Antagonist Radioligand Binding in Membranes from Whole Brain or Spinal Cord of Wild-Type and Gαo Transgenic Mice.
Tissue | Genotype |
[3H]DPN binding |
[3H]DAMGO binding |
||
---|---|---|---|---|---|
Total (fmol/mg protein) | MOR (fmol/mg protein)a | Bmax (fmol/mg protein) | KD (nM) | ||
Whole brain | Wild type | 366±24 | 218±13b | 246±29 | 2.5±0.4 |
Gαo +/− | 391±38 | 216±3 | 181±16 | 1.9±0.5 | |
Gαo −/− | 407±38 | 233±12 | 121±17* | 3.5±1.3 | |
Spinal cord | Wild type | 161±20 | 95±5 | 84±5c | ND |
Gαo +/− | 161±14 | 101±6 | 93±6c | ND |
Abbreviation: ND, not determined.
MOR expression was evaluated as the amount of bound [3H]DPN at a maximal concentration that was displaced by the MOR-selective antagonist CTAP (300 nM).
In wild-type whole brain, there is a trend for total MOR to be less than high-affinity MOR because binding was measured indirectly (see Materials and Methods).
In spinal cord, Bmax values were estimated using a single maximal concentration of [3H]DAMGO.
Data represent the mean±SEM (n=2–3 performed in at least duplicate). Asterisk indicates a statistical difference vs wild-type whole brain by Bonferroni's post-test (p<0.05).