Table 2. The binding of conjugates of aminoadamantanes with carbazole derivatives C-1 and C-2 (Fig. 1) to МК-801 and ifenprodil binding sites of NMDA receptor.
Compounds |
Binding characteristics of compounds |
||||||
---|---|---|---|---|---|---|---|
No | R | R1 | R2 | % of [3H]МК-801 blockade at 100 μM of compound | [3H]МК-801, IC50, μM | % of [3H]ifenprodil blockade at 100 μM of compound | [3H]ifenprodil, IC50, μM |
C-1a | H | H | H | 83.5 ± 7.6 | 75.3 ± 6.9 | 74.2 ± 6.8 | 8.2 ± 0.8 |
C-1b | H | H | CH3 | 68.5 ± 5.4 | 59.1 ± 4.9 | 76.2 ± 6.6 | 21.3 ± 1.9 |
C-1c | Br | Br | H | 55.1 ± 4.9 | 79.4 ± 7.5 | 85.3 ± 7.6 | 22.9 ± 1.8 |
C-1d | Br | Br | CH3 | 33.8 ± 3.5 | >100 | 67.6 ± 5.8 | 31.5 ± 3.3 |
C-1e | CI | CI | H | 28.3 ± 1.8 | >100 | 70.6 ± 7.1 | 21.8 ± 1.8 |
C-1f | CI | CI | CH3 | 72.8 ± 6.8 | 22.4 ± 2.1 | 71.4 ± 5.7 | 14.6 ± 1.5 |
C-2a | H | H | H | 32.3 ± 3.0 | >100 | 71.6 ± 8.3 | 82.5 ± 9.3 |
C-2b | H | H | CH3 | 62.2 ± 6.3 | 14.2 ± 2.3 | 58.4 ± 5.6 | 65.5 ± 6.1 |
C-2c | CH3 | H | H | 0 ± 2.0 | >100 | 51.6 ± 7.2 | 98.4 ± 6.9 |
C-2d | CH3 | H | CH3 | 18.3 ± 2.0 | >100 | 31.4 ± 3.1 | >100 |
C-2e | CH3 | CH3 | H | 29.3 ± 6.4 | >100 | 67.2 ± 7.3 | 8.1 ± 1.7 |
C-2f | CH3 | CH3 | CH3 | 65.2 ± 5.3 | 19.5 ± 1.6 | 71.4 ± 6.5 | 10.3 ± 1.9 |
C-2g | F | H | H | 0 ± 2.0 | >100 | 48.4 ± 5.2 | >100 |
C-2h | F | H | CH3 | 88.5 ± 9.0 | 27.4 ± 4.1 | 87.2 ± 7.3 | 10.4 ± 2.9 |
Memantine | 100 | 1.36 ± 0.086 | 11.2 ± 1.1 | >100 | |||
Amantadine | 57.2 ± 5.5 | 35.5 ± 3.2 | 44.6 ± 4.6 | >100 |