季铵化合物对红细胞中胆碱转运的影响。

Effects of quaternary ammonium compounds on choline transport in red cells.

作者信息

Martin K

出版信息

Br J Pharmacol. 1969 Jul;36(3):458-69. doi: 10.1111/j.1476-5381.1969.tb08002.x.

DOI:10.1111/j.1476-5381.1969.tb08002.x

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1703621/

Abstract

Neuromuscular blocking agents have been shown to be powerful inhibitors of choline transport in human erythrocytes. Ganglionic blocking agents were weaker inhibitors.2. The affinity of the choline transport site for alkyltrimethylammonium compounds was considerably higher than its affinity for alkyl-bis-(trimethylammonium) compounds of similar chain length. The affinity increases with increasing length of the alkyl chain in both series.3. Tetramethylammonium (TMA), ethyl- and propyltrimethylammonium appear to enter the cells on the choline carrier while the larger monoquaternary compounds, and the bisquaternary compounds, bind to the carrier but are unable to cross the cell membrane.4. Radioactively labelled carbachol, acetylcholine and decamethonium do not enter the cells on the choline carrier.5. Choline transport in erythrocytes from patients with myasthenia gravis is normal, suggesting that this disorder is not associated with a generalized defect of choline transport.

摘要

神经肌肉阻滞剂已被证明是人类红细胞中胆碱转运的强力抑制剂。神经节阻滞剂是较弱的抑制剂。
胆碱转运位点对烷基三甲基铵化合物的亲和力明显高于对链长相似的烷基双（三甲基铵）化合物的亲和力。在这两个系列中，亲和力都随着烷基链长度的增加而增加。
四甲基铵（TMA）、乙基和丙基三甲基铵似乎通过胆碱载体进入细胞，而较大的单季铵化合物和双季铵化合物与载体结合但无法穿过细胞膜。
放射性标记的卡巴胆碱、乙酰胆碱和十烃季铵不会通过胆碱载体进入细胞。
重症肌无力患者红细胞中的胆碱转运正常，这表明这种疾病与胆碱转运的普遍缺陷无关。