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- W2093566453 abstract "The GABA-inhibitory action of bicuculline on lobster muscle was critically re-examined. Bicuculline (20–100 μM) depressed the GABA-evoked conductance increase in a reversible manner, the double reciprocal transformation of the GABA dose/conductance curves remaining linear. If bicuculline was assumed to be a pure non-competitive antagonist, then the observed depression of the GABA curves at high GABA concentrations was underestimated. Also, the action of bicuculline was not in accordance with a dualistic antagonism (competitive and pure non-competitive type). Regarding bicuculline as a ‘mixed’ non-competitive antagonist however, gave a better overall fit to the experimental data. Combinations of bicuculline and picrotoxinin also depressed the GABA response in a manner expected from the combination of two ‘mixed’ non-competitive antagonists. It was concluded that bicuculline (like picrotoxinin and picrotoxin) behaves as a ‘mixed’ non-competitive rather than a pure non-competitive antagonist of GABA on lobster muscle. However bicuculline methochloride proved inactive on the lobster. Moreover, bicuculline itself became less effective in a more acidic solution (pH 5.6, where more of the protonated form would exist). An intracellular or intramembrane site of action of this antagonist was therefore postulated." @default.
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- W2093566453 date "1981-03-01" @default.
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- W2093566453 title "A re-examination of the gaba-inhibitory action of bicuculline on lobster muscle" @default.
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- W2093566453 doi "https://doi.org/10.1016/0014-2999(81)90428-3" @default.
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