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. 2017 Mar 30;7:45627. doi: 10.1038/srep45627

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