Table 3 The binding of γ-carboline-phenothiazine conjugates (Fig. 1) to МК-801 and ifenprodil binding sites of NMDA receptor.
Compounds | Binding characteristics of compounds | |||||
|---|---|---|---|---|---|---|
No | R1 | R2 | % of [3H]MK-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 | CH3 | CH3 | 80.4 ± 6.6 | 13.5 ± 3.6 | 42.6 ± 7.2 | 88.4 ± 8.3 |
C-1b | CH3 | С2H5 | 95.7 ± 1.0 | 8.5 ± 0.8 | 48.1 ± 5.9 | 74.4 ± 4.0 |
C-1c | F | CH3 | 78.7 ± 1.4 | 17.7 ± 2.6 | 50.2 ± 5.2 | 55.1 ± 5.8 |
C-1d | H | CH3 | 74.9 ± 1.1 | 18.5 ± 0.9 | 60.1 ± 1.4 | 23.4 ± 0.7 |
C-1e | H | С2H5 | 76.1 ± 1.2 | 14.6 ± 1.9 | 69.4 ± 3.3 | 13.4 ± 2.6 |
C-1f | F | С2H5 | 82.4 ± 7.3 | 15.8 ± 1.8 | 78.2 ± 6.8 | 8.8 ± 1.8 |
C-1g | С2H5 | CH3 | 89.4 ± 4.6 | 13.2 ± 2.2 | 64.6 ± 5.2 | 15.4 ± 3.9 |
C-1h | i-С3H7 | CH3 | 80.3 ± 6.9 | 17.8 ± 2.0 | 88.7 ± 5.6 | 85.8 ± 7.2 |
C-2a | CH3 | CH3 | 87.1 ± 7.7 | 84.8 ± 9.2 | 69.7 ± 8.3 | 57.2 ± 6.7 |
C-2b | F | С2H5 | 24.1 ± 1.9 | 106.3 ± 9.2 | 25.7 ± 4.6 | 81.2 ± 6.7 |
C-2c | CH3O | CH3 | 19.1 ± 2.2 | 113.4 ± 11.1 | 47.4 ± 6.6 | 115.4 ± 9.3 |
dimebon | 27.8 ± 3.9 | 91.5 ± 7.7 | 34.1 ± 4.9 | 82.4 ± 4.1 | ||
МB | 2.0 ± 4.0 | n/d | 70.4 ± 10.1 | 9.3 ± 4.5 | ||
