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Updated: May 15, 2025

Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
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人类α7尼古丁乙胆受体的全性激动的结构基础

Sanling Liu1,2, Yining Zheng3, Haopeng Chen3

  • 1Division of Life Sciences and Medicine, Joint Center for Biological Analytical Chemistry, Anhui Engineering Laboratory of Peptide Drug, University of Science and Technology of China, Hefei, Anhui, China. sanling@ustc.edu.cn.

Cell discovery
|April 8, 2025
PubMed
概括

这项研究揭示了GAT107,ago-PAM和如何通过结构变化调节α7尼古丁乙胆受体 (nAChR). 这一发现为药物设计的nAChR门机制提供了新的见解.

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Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
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The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
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