Fig. 4.

TETS remains pharmacodynamically active in vivo for 14 days. a Pooled serum from mice sacrificed 2 days or 14 days after administration of 0.2 mg/kg TETS blocks current through recombinantly expressed α₂β₃γ₂ GABA_A receptors. Control currents were elicited by 40 μM GABA, which corresponds to the EC₉₀ for this receptor combination. After washout, serum extracts were perfused and currents again elicited by 40 μM GABA. Only recordings where TETS could subsequently be washed out were used for quantification of the blocking effect. Control serum: 1.3 ± 4.2% (n = 5 cells); 1 μM TETS: 60.5 ± 4.4% current block (n = 8 cells); pooled 2-day serum: 61.3 ± 9.4% current block (n = 4 cells); pooled 14-day serum: 39.4 ± 8.3% current block (n = 7 cells). Data are mean ± SD. Inhibition of GABA currents by extracts from mouse brain removed 10 min (b) and 2 days (c) after TETS administration