Table 3.
Inhibition of [35S]TBPS binding by TBPS, picrotoxin, GABA, loreclezole and pentobarbital in postmortem human and rat cortex and cerebellum membranes
Human brain |
Rat brain |
|||||||
---|---|---|---|---|---|---|---|---|
Cortex |
Cerebellum |
Cortex |
Cerebellum |
|||||
IC50 (μM) | Hill slope | IC50 (μM) | Hill slope | IC50 (μM) | Hill slope | IC50 (μM) | Hill slope | |
TBPS | 0.054±0.009* | 0.86±0.15 | 0.046±0.012* | 1.18±0.23 | 0.021±0.005 | 0.91±0.07 | 0.022±0.005 | 0.95±0.02 |
Picrotoxin | 0.31±0.03* | 0.84±0.02 | 0.43±0.06* | 0.87±0.11 | 0.18±0.04 | 0.85±0.03 | 0.18±0.03 | 0.87±0.03 |
GABA | 0.90±0.07 | 1.35±0.05 | 0.65±0.11 | 1.24±0.17 | 1.13±0.15 | 1.56±0.14 | 0.90±0.08 | 1.21±0.08 |
Loreclezole | 21±7* | 0.88±0.09 | 12±4* | 0.90±0.11 | 8.4±1.8 | 0.83±0.06 | 5.0±0.9 | 0.99±0.08 |
Pentobarbital | 177±42* | 1.11±0.13 | 110±25* | 1.08±0.05 | 64±9 | 1.14±0.05 | 58±10 | 1.11±0.06 |
Abbreviations: GABA, γ-aminobutyric acid; [35S]TBPS, [35S]t-butylbicyclophosphorothionate; TBPS, t-butylbicyclophosphorothionate.
Data shown are mean±s.e.m. (n=3–4).
P<0.05; comparison with corresponding rat tissue using an unpaired t-tests.