Neuronal nicotinic acetylcholine receptors (nnAChRs) are members of the ligand-gated ion channel superfamily, and widely expressed in the central and peripheral nervous systems with many subunits. NnAChRs have been represented novel targets for a wide variety of therapeutic agents based on their complex functions. It is known that both central and peripheral nnAChRs are sensitive to various types of general anesthetics, among those, barbiturates, ketamine, volatile and gaseous anesthetics depress nnAChRs at or below clinical concentrations. It is possible that inhibition of nnAChRs is one of factors involved in the mechanisms of general anesthesia.
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Toxins (Basel)
November 2024
Institut des Neurosciences Paris-Saclay, UMR 9197, CNRS/Université Paris-Sud, 91198 Gif-sur-Yvette, Cedex, France.
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Department of Applied Chemistry and Life Sciences, Graduate School of Engineering, Toyohashi University of Technology, Toyohashi, Aichi 441-8580, Japan; Center for Diversity and Inclusion, Toyohashi University of Technology, Toyohashi, Aichi, 441-8580, Japan. Electronic address:
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January 2025
Department of Immunology, Genetics and Pathology, Uppsala University, Uppsala, Sweden.
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March 2024
School of Basic Medicine, Heilongjiang University Of Chinese Medicine, Harbin, 150040, China.
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Department of Molecular Neuroimmune Signaling, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 16/10 Miklukho-Maklay Str., 117997 Moscow, Russia. Electronic address:
Non-conventional snake venom toxins, such as WTX from the cobra Naja kaouthia, are three-finger proteins containing a fifth disulfide bond in the N-terminal polypeptide loop I and inhibiting α7 and muscle-type nicotinic acetylcholine receptors (nAChRs). Because the central polypeptide loop II of non-conventional toxins plays an important role in their biological activity, we synthesized several WTX loop II fragments with two cysteine residues added at the N- and C-termini and oxidized to form a disulfide bond. The inhibition by peptides of several nAChRs subtypes was investigated using different methods and the effects of peptides on the rat arterial pressure and heart rate were analyzed.
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