Table 2. Binding affinity of D-473 for CNS receptors.
| Target Receptor | Radioligand | % Inhibition of Binding at 10 µM D-473 | Ki for D-473(nM) |
| D1 | [3H]SCH 23390 | 62.2 | 630 |
| D2 | [3H]N-methylspiperone | 42.9 | |
| D3 | [3H]N-methylspiperone | 30.8 | |
| D4 | [3H]N-methylspiperone | 37.2 | |
| D5 | [3H]SCH 23390 | 74.7 | 1571 |
| 5HT1a | [3H]8-OH-DPAT | 35.4 | |
| 5HT1b | [3H]GR-125743 | 14.2 | |
| 5HT1e | [3H]5-HT | 38 | |
| 5HT1d | [3H]GR-125743 | 39 | |
| 5HT2a | [3H]ketanserin | 16.3 | |
| 5HT2b | [3H]LSD | 70.8 | 597 |
| 5HT2c | [3H]Mesulergine | 45.4 | |
| 5HT3 | [3H] LY 278,584 | 3.5 | |
| 5HT5a | [3H]LSD | 19.5 | |
| 5HT6 | [3H]LSD | −11.4 | |
| 5HT7 | [3H]LSD | 41.4 | |
| GABA A | [3H]Muscimol | 5.1 | |
| Alpha1A | [3H]Prazosin | 23.6 | |
| Alpha1B | [3H]Prazosin | 16.6 | |
| Alpha1D | [3H]Prazosin | 41.8 | |
| Alpha2A | [3H]Clonidine | 14.5 | |
| Alpha2B | [3H]Clonidine | 25.4 | |
| Alpha2C | [3H]Clonidine | 61 | >10,000 |
| Beta1 | [125I]Iodopindolol | 24.6 | |
| Beta2 | [125I]Iodopindolol | −4.4 | |
| Beta3 | [125I]Iodopindolol | 61.2 | >10,000 |
| BZP Rat Brain Site | 3H-Flunitrazepam | −3 | |
| δ-opioid | [3H]DADLE | 42.7 | |
| κ-opioid | [3H]Bremazocine | 48.5 | |
| H1 | [3H]Pyrilamine | 2.8 | |
| H2 | [3H]Tiotodine | 70.1 | 141 |
| H3 | [3H]Alpha-methyl Histamine | −14.7 | |
| µ-Opioid | [3H]Diprenorphine | 20.5 | |
| M1 | [3H]QNB | 15 | |
| M2 | [3H]QNB | −9.5 | |
| M3 | [3H]QNB | 6.9 | |
| M4 | [3H]QNB | −16.7 | |
| M5 | [3H]QNB | 3.2 | |
| PBR | 8.4 |
The default concentration of drugs for primary binding experiments was 10 µM, and % inhibition (mean of 4 determinations) is shown. Except where indicated assays were with heterologous expression systems. Study was carried out by the National Institute of Mental Health’s Psychoactive Drug Screening Program.