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Muscarinic toxins: tools for the study of the pharmacological and functional properties of muscarinic receptors
Author(s) -
Servent Denis,
FruchartGaillard Carole
Publication year - 2009
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.2009.06092.x
Subject(s) - muscarinic acetylcholine receptor , muscarinic acetylcholine receptor m4 , muscarinic acetylcholine receptor m1 , muscarinic acetylcholine receptor m5 , muscarinic acetylcholine receptor m3 , metabotropic receptor , muscarinic acetylcholine receptor m2 , acetylcholine , neuroscience , pharmacology , acetylcholine receptor , biology , receptor , chemistry , biochemistry , agonist
Muscarinic receptors mediate metabotropic actions of acetylcholine in the CNS and PNS and autocrine functions of acetylcholine in non‐neuronal systems. Because of the lack of highly selective muscarinic ligands, the precise location, functional role, and roles in various diseases of the five muscarinic receptor subtypes remain unclear. Muscarinic toxins isolated from the venom of Dendroaspis snakes have a natural high affinity and selectivity, associated with roles as competitive antagonists, allosteric modulators, and potential agonists. These toxins may therefore be invaluable tools for studying muscarinic receptors. We review data on the structural and pharmacological characterization of the muscarinic toxins, focusing on recent structure–function studies on toxin–receptor interactions. We discuss the potential benefits of using these toxins for investigating muscarinic function in vivo .