Kobayashi H, Yuyama A, Matsusaka N, Takeno K, Yanagiya I
J Toxicol Sci. 1979 Nov;4(4):351-62. doi: 10.2131/jts.4.351.
The effects of methylmercury chloride and other mercury compounds on cholinergic parameters were studied in vitro. Methylmercury chloride (MMC) and phenylmercury acetate inhibited choline acetyltransferase (ChA) with 20 microM of I50, and mercury nitrate (MN) with 100 microM of I50. All the three compounds had little effect on cholinesterase activity. MMC inhibited a high affinity choline uptake with 41 microM of Ki, as well as a low affinity choline uptake with 250 microM of Ki. MMC did not affect a spontaneous and potassium-stimulated ACh release from brain tissue slices incubated in eserinized Krebs-Ringer's solution up to the concentration of 100 microM. It was shown that the organic mercury compounds, such as methylmercury, were potent inhibitors of the choline uptake systems, as well as ChA activity.
在体外研究了氯化甲基汞和其他汞化合物对胆碱能参数的影响。氯化甲基汞（MMC）和醋酸苯汞对胆碱乙酰转移酶（ChA）的抑制作用，半数抑制浓度（I50）为20微摩尔，硝酸汞（MN）的I50为100微摩尔。这三种化合物对胆碱酯酶活性几乎没有影响。MMC对高亲和力胆碱摄取的抑制常数（Ki）为41微摩尔，对低亲和力胆碱摄取的Ki为250微摩尔。在加入毒扁豆碱的 Krebs-Ringer 溶液中孵育的脑组织切片，当MMC浓度高达100微摩尔时，对乙酰胆碱（ACh）的自发释放和钾刺激释放均无影响。结果表明，有机汞化合物，如甲基汞，是胆碱摄取系统以及ChA活性的有效抑制剂。
