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- W2045831795 abstract "We established [V. I. Fetisov et al., J. Fluorine Chem., 54 (1991) 301] that compounds ( I, II ) possessed gamma-aminobutyric (GABA)-antagonistic properties. In this contribution we present data on the influence of I and II on the GABA induced Cl − currents by two in vitro methods: A. the 36 Cl − traced uptake into rat brain synapto-neurosomes; B. registration under the voltage clamp and perfusion of total current in the neurons of Limnea Stagnalis (fresh water molluscian; Cl − nature of currents proved). The aim of this investigations is to compare I and II with others types of ‘cage’ convulsantspricrotoxin ( PCT ) and bicyclophosphate III . The results we obtained and compiled in the table are: IC 50 (nM) — concentration at which Cl − uptake is inhibited by 50%; percentage of the total current inhibition at the conc. used (mcM); LD 50 -toxicity, mice, i.p., mg/kg. Method I II PCT III A.IC5 50 , nM 61.0 5.32 360 1.09 B.%/mcM 22.6/10 40.9/0.1 40/1.0 - LD 50 1.0 0.1 3.0 0.38 The correlation between IC 50 and LD 50 is good (r = 0.99) although some discrepancy exists for III being more active than II in vitro but not in vivo . Thus, I and II are similar to PCT ." @default.
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- W2045831795 date "1992-08-01" @default.
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- W2045831795 title "Fluoro-containing ‘cage’ convulsants: inhibition of gamma-aminobutyric acid induced Cl−currents" @default.
- W2045831795 doi "https://doi.org/10.1016/s0022-1139(00)80833-7" @default.
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