胆碱的一些环状类似物的药理作用。
Pharmacological actions of some cyclic analogues of choline.
作者信息
Hemsworth B A, Shreeve S M, Veitch G B
出版信息
Br J Pharmacol. 1984 Apr;81(4):685-92. doi: 10.1111/j.1476-5381.1984.tb16135.x.
Two cyclic choline analogues (3-hydroxy-N,N- dimethylpiperidinium and 2-hydroxymethyl-N,N- dimethylpiperidinium ) and two cyclic homocholine analogues (4-hydroxy-N,N- dimethylpiperidinium and 3-hydroxymethyl-N,N- dimethylpiperidinium ) have been studied with regard to their actions at the cholinergic synapse. All the analogues had some direct depolarizing activity on the frog rectus abdominis muscle but they were less potent in this respect than acetylcholine. Compared to physostigmine, the analogues were weak inhibitors of cholinesterase enzymes. All the analogues were found to have a presynaptic blocking action on the rat phrenic nerve-hemidiaphragm preparation, which was reversed by choline. In addition, they all inhibited the high affinity transport of choline into synaptosomes but only the cyclic choline analogues were found to be acetylated by soluble choline acetyltransferase in vitro. We conclude that the hydroxypiperidinium analogues caused the presynaptic block seen at the neuromuscular junction by inhibiting acetylcholine synthesis.
已对两种环状胆碱类似物（3-羟基-N,N-二甲基哌啶鎓和2-羟甲基-N,N-二甲基哌啶鎓）以及两种环状高胆碱类似物（4-羟基-N,N-二甲基哌啶鎓和3-羟甲基-N,N-二甲基哌啶鎓）在胆碱能突触处的作用进行了研究。所有类似物对青蛙腹直肌均有一定的直接去极化活性，但在这方面它们的效力比乙酰胆碱弱。与毒扁豆碱相比，这些类似物是胆碱酯酶的弱抑制剂。发现所有类似物对大鼠膈神经-半膈肌标本均有突触前阻断作用，胆碱可使其逆转。此外，它们均抑制胆碱向突触体的高亲和力转运，但仅环状胆碱类似物在体外可被可溶性胆碱乙酰转移酶乙酰化。我们得出结论，羟基哌啶鎓类似物通过抑制乙酰胆碱合成导致了在神经肌肉接头处观察到的突触前阻断。
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