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. 2013 Apr 25;169(2):371–383. doi: 10.1111/bph.12151

Figure 4.

Figure 4

Pyrazoloquinolinones/ pyrazolopyridinones exhibiting either weak or no affinity for the benzodiazepine binding site exert their action via the α1+β3− binding site (A) Effects of compound 32, or (B) compound 8, on α1β3 (▪), or on α1β3 pre-incubated with MTSEA-biotin(□) and, on α1V211Cβ3Q64C (•) receptors or α1V211Cβ3Q64C (MB), receptors labelled by MTSEA-biotin (○). A significant reduction of the effects of compound 32 or compound 8 was only observed in mutated receptors labelled with MTSEA-biotin (α1V211Cβ3Q64C MB) (at 1 μM P < 0.05; at 3, 10 and 30 μM P < 0.001 for both compounds). Data represent means ± SEM (n = 5–6). (C) The positive modulatory effects of 3 μM compound 32 (345 ± 32), or (D) of 10 μM compound 8 (211 ± 10) on GABA EC3 could be concentration-dependently inhibited by compound 33, an α+/β− binding site null modulator. Data represent means ± SEM (n = 4–5).