Effects of triethyl lead on various cholinergic parameters in the rat brain in vitro.
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概要
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The effects of triethyl lead acetate (triethyl Pb) on the cholinergic system in the brain of the rats were investigated in vitro. Triethyl Pb, at concentrations below 10<SUP>-4</SUP> M, inhibited the depolarized release of acetylcholine (ACh) from slices of cortex and they synthesis of ACh in such slices, while it potentiated in a dose-dependent manner the non-depolarized release of ACh. In contrast, lead inhibited noncompetitively the high-affinity uptake of choline into synaptosomes with a K<SUB>i</SUB> of 4.03 × 10<SUP>-6</SUP> M and the activity of choline acetyltransferase with a K<SUB>i</SUB> of 4.07 × 10<SUP>-5</SUP> M. Triethyl Pb has an inhibitory effect (IC<SUB>50</SUB> ≈ 5 × 10<SUP>-5</SUP> M) on the binding of [<SUP>3</SUP>H]quinuclidinyl benzilate to muscarinic ACh receptors. Triethyl Pb inhibited acetylcholinesterase activity slightly at 5 × 10<SUP>-5</SUP> and 10<SUP>-4</SUP> M. It is suggested that ACh transmission, in particular the synthesis of ACh and the release of ACh, is susceptible to organolead neurotoxicity.
- 公益社団法人 日本薬理学会の論文
著者
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Hoshi Fumio
Department Of Small Animal Internal Medicine School Of Veterinary Medicine Kitasato University
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Yuyama Akira
Department Of Animal Husbandry Faculty Of Agriculture Tohoku University
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Matsusaka Naonori
Department Of Veterinary Medicine Faculty Of Agriculture Iwate University
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KOBAYASHI HARUO
Department of Animal Breeding, Faculty of Agriculture, University of Tokyo
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