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  • 标题:Macromolecules from Lobster Axon Membranes That Bind Cholinergic Ligands and Local Anesthetics
  • 本地全文:下载
  • 作者:Jeffrey L. Denburg ; Mohyee E. Eldefrawi ; Richard D. O'Brien
  • 期刊名称:Proceedings of the National Academy of Sciences
  • 印刷版ISSN:0027-8424
  • 电子版ISSN:1091-6490
  • 出版年度:1972
  • 卷号:69
  • 期号:1
  • 页码:177-181
  • DOI:10.1073/pnas.69.1.177
  • 语种:English
  • 出版社:The National Academy of Sciences of the United States of America
  • 摘要:The technique of reversible equilibrium dialysis has been applied to the study of macromolecules that are essential for axonal conduction. A binding component from a preparation of an axon-plasma membrane has been characterized and shown to bind nicotine with a KD = 0.42 {+/-} 0.04 {micro}M and to the extent of 0.7 nmol/g of wet nerve. This binding was competitively blocked by acetylcholine (Ki = 43 {+/-} 7 {micro}M) and procaine (Ki = 2.9 {+/-} 0.2 {micro}M). This axonal macromolecule exhibits several of the properties of cholinergic postsynaptic receptors including its concentration in the tissue, blockade of its binding of nicotine by cholinergic drugs and [α]-bungarotoxin, and its phospholipoprotein nature. Some important differences are a lower affinity for acetylcholine and its binding of procaine. It is suggested that this nicotine receptor is on the internal surface of the axon plasma membrane and is a component common to both the Na+ and K+ gates.
  • 关键词:receptors ; procaine ; acetylcholine ; nicotine ; Na+ and K+ gates
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