Hemsworth B A, Shreeve S M, Veitch G B
Br J Pharmacol. 1984 Jun;82(2):477-84. doi: 10.1111/j.1476-5381.1984.tb10783.x.
A cyclic choline analogue, 3-hydroxy-N,N-dimethylpiperidinium, has been shown to be transported into a crude preparation of synaptosomes by high and low affinity transport mechanisms. Under conditions favouring the high affinity system the synaptosomes metabolized approximately 50% of the accumulated analogue to 3-acetoxy-N,N-dimethylpiperidinium, which was detected by paper electrophoresis. The phrenic nerve endplate region of a mouse hemidiaphragm accumulated 3-hydroxy-N,N-dimethylpiperidinium on nervous stimulation. This tissue metabolized approximately 60% of the accumulated analogue to the acetylated derivative which was released on nervous stimulation into the bathing medium. Compared to acetylcholine, 3-acetoxy-N,N-dimethylpiperidinium was shown to be 57 times less potent an agonist at the nicotinic receptors of the frog rectus abdominis muscle and 162 times less potent an agonist at the muscarinic receptors of the guinea-pig ileum. It is concluded that 3-hydroxy-N,N-dimethylpiperidinium is a precursor of a false cholinergic transmitter.
一种环状胆碱类似物，即3-羟基-N，N-二甲基哌啶鎓，已被证明可通过高亲和力和低亲和力转运机制转运至突触体粗制品中。在有利于高亲和力系统的条件下，突触体将约50%积累的类似物代谢为3-乙酰氧基-N，N-二甲基哌啶鎓，通过纸电泳检测到该物质。小鼠半膈的膈神经终板区域在神经刺激时积累3-羟基-N，N-二甲基哌啶鎓。该组织将约60%积累的类似物代谢为乙酰化衍生物，该衍生物在神经刺激时释放到浴液中。与乙酰胆碱相比，3-乙酰氧基-N，N-二甲基哌啶鎓在青蛙腹直肌烟碱受体上作为激动剂的效力低57倍，在豚鼠回肠毒蕈碱受体上作为激动剂的效力低162倍。得出的结论是，3-羟基-N，N-二甲基哌啶鎓是一种假性胆碱能递质的前体。
