Table 2.
Binding affinity of D-142 for CNS receptors. The default concentration of drugs for primary binding experiments was 10 μM, and % inhibition (mean of 4 determinations) is shown.
| Target Receptor | Radioligand | % Inhibition of Binding at 10 μM D-142 | Ki for D-161 (nM) |
|---|---|---|---|
| D1 | [3H]SCH 23390 | 2.5 | |
| D2 | [3H]N-methylspiperone | 3.2 | |
| D3 | [3H]N-methylspiperone | 15.3 | |
| D4 | [3H]N-methylspiperone | 3.1 | |
| D5 | [3H]SCH 23390 | 17.2 | |
| 5HT1a | [3H]8-OH-DPAT | 45.9 | |
| 5HT1b | [3H]GR-125743 | 9.1 | |
| 5HT1e | [3H]5-HT | 3.4 | |
| 5HT1d | [3H]GR-125743 | -6.2 | |
| 5HT2a | [3H]ketanserin | 12.7 | |
| 5HT2b | [3H]LSD | 46.3 | |
| 5HT2c | [3H]Mesulergine | 30.6 | |
| 5HT3 | [3H] LY 278,584 | 18 | |
| 5HT5a | [3H]LSD | 22.5 | |
| 5HT6 | [3H]LSD | 8.7 | |
| 5HT7 | [3H]LSD | 15.6 | |
| GABAA | [3H]Muscimol | 0.6 | |
| Alpha1A | [3H]Prazosin | 51.6 | >10,000 |
| Alpha1B | [3H]Prazosin | 24.8 | |
| Alpha1D | [3H]Prazosin | 30 | |
| Alpha2A | [3H]Clonidine | 45.8 | |
| Alpha2B | [3H]Clonidine | 28.5 | |
| Alpha2C | [3H]Clonidine | 32.9 | |
| Beta1 | [125I]Iodopindolol | -4.7 | |
| Beta2 | [125I]Iodopindolol | -3.8 | |
| Beta3 | [125I]Iodopindolol | 60.7 | >10,000 |
| BZP Rat Brain Site | 3H-Flunitrazepam | 20.5 | |
| Ca2+ Channel | [3H]Nitrendipine | 3.1 | |
| δ-opioid | [3H]DADLE | 3.3 | |
| κ-opioid | [3H]Bremazocine | 54.3 | 721 ± 70.28 |
| H1 | [3H]Pyrilamine | -16.9 | |
| H2 | [3H]Tiotodine | 100 | 90 ± 7 |
| H3 | [3H]Alpha-methyl Histamine | 3 | |
| H4 | [3H]Histamine | -13.7 | |
| μ-Opioid | [3H]Diprenorphine | 48.8 | |
| M1 | [3H]QNB | -1.7 | |
| M2 | [3H]QNB | 23 | |
| M3 | [3H]QNB | -3.1 | |
| M4 | [3H]QNB | -3.4 | |
| M5 | [3H]QNB | 16 | |
| NMDA PCP Site | MK801 | 15.4 |