|
Characterization of compounds by heterologous competition binding |
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| Compound |
pKi |
|||||
|
|
||||||
| hD1 |
hD2L |
hD3 |
hD4.4 |
hD5 |
h5HT2A |
|
|
|
||||||
| Haloperidol |
6.55 ± 0.09 |
8.56 ± 0.05 |
8.00 ± 0.05 |
8.10 ± 0.04 |
7.50 ± 0.06 |
6.84 ± 0.12 |
| Clozapine |
6.68 ± 0.03 |
6.60 ± 0.06 |
6.13 ± 0.05 |
6.93 ± 0.08 |
6.50 ± 0.08 |
8.23 ± 0.07 |
| LE300 |
7.98 ± 0.06 |
7.19 ± 0.04 |
6.48 ± 0.04 |
6.46 ± 0.08 |
7.99 ± 0.05 |
9.65 ± 0.04 |
| LE400 |
5.58 ± 0.16 |
5.90 ± 0.05 |
5.28 ± 0.07 |
4.79 ± 0.06 |
5.44 ± 0.07 |
6.86 ± 0.13 |
| LE401 |
4.77 ± 0.25 |
5.06 ± 0.13 |
4.83 ± 0.16 |
< 4a) |
4.79 ± 0.50 |
< 4a) |
| LE403 |
7.94 ± 0.06 |
6.43 ± 0.07 |
6.14 ± 0.10 |
6.26 ± 0.06 |
7.84 ± 0.05 |
8.40 ± 0.08 |
| LE404 |
8.47 ± 0.10 |
7.10 ± 0.05 |
6.73 ± 0.06 |
7.23 ± 0.03 |
8.53 ± 0.09 |
8.79 ± 0.07 |
| LE410 |
7.76 ± 0.04 |
7.54 ± 0.06 |
6.86 ± 0.07 |
6.32 ± 0.06 |
7.78 ± 0.10 |
8.40 ± 0.10 |
| LE420 |
6.89 ± 0.07 |
6.64 ± 0.05 |
6.07 ± 0.06 |
5.83 ± 0.11 |
6.92 ± 0.04 |
7.97 ± 0.05 |
|
a) Displacement of radioligand was < 30% at 10 μM Haloperidol, clozapine, and LE compounds were characterized at dopamine and h5HT2A receptors. [3H]SCH23390 was used for hD1-like and [3H]spiperone for hD2-like and h5HT2A receptors. Displayed are pKi values ± SEM, n ≥ 3. | ||||||
Hamacher et al. BMC Pharmacology 2006 6:11 doi:10.1186/1471-2210-6-11 |
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