Table 1.
DKR-1677 Binding Profile at Non-Sigma Receptor Sitesa
| target | Ki (nM) | target | Ki (nM) |
|---|---|---|---|
| 5HT1A | 1187 | Beta2 | >10 000 |
| 5HT1B | >10 000 | Beta3 | >10 000 |
| 5HT1D | 1913 | BZP rat brain | 4767 |
| 5HT1e | 7741 | D1 | >10 000 |
| 5HT2A | 1274 | D2 | >3253 |
| 5HT2B | 868 | D3 | 4426 |
| 5HT2C | 2138 | D4 | >10 000 |
| 5HT3 | >10 000 | D5 | 4888 |
| 5HT5a | 3238 | DAT | 2080 |
| 5HT6 | 2510 | DOR | >10 000 |
| 5HT7 | 766 | GabaA | >10 000 |
| A2B2 | b | H1 | 100 |
| A2B4 | b | H2 | 1766 |
| A3B2 | b | H3 | 644 |
| A3B4 | b | H4 | >10 000 |
| A4B2 | b | hERG | 695 |
| A4B2c | b | KOR | 8515 |
| A4B4 | b | M1 | 4062 |
| A7 | b | M2 | 4326 |
| A7c | b | M3 | 1114 |
| Alpha1a | 2667 | M4 | 1634 |
| Alpha1b | >10 000 | M5 | 1395 |
| Alpha1d | 1905 | MOR | 8798 |
| Alpha2a | 340 | NET | 3845 |
| Alpha2b | 1799 | NMDA | 10 000 |
| Alpha2c | 539 | PBR | >10 000 |
| Beta1 | 6282 | SERT | 8630 |
a
Receptor binding assays were performed by the Psychoactive Drug Screening Program (PDSP)at Chapel Hill, North Carolina. The assay protocol book can be accessed free of charge at: https://pdspdb.unc.edu/pdspWeb/content/PDSP%20Protocols%20II%202013-03-28.pdf. Values represented are single Ki determination.
b
<50% inhibition of radioligand binding at 10 μM.
c
Sourced from rodent brain.