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Radioligand Binding at Muscarinic Receptors

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Muscarinic Receptor: From Structure to Animal Models

Part of the book series: Neuromethods ((NM,volume 107))

Abstract

Five subtypes of muscarinic acetylcholine receptors denoted M1 through M5 have been cloned. Muscarinic receptors mediate a wide array of physiological functions and impairment of muscarinic signaling is involved in numerous pathological conditions including Alzheimer’s disease and schizophrenia. Reliable radioligand binding techniques allow study of involvement of individual muscarinic receptor subtypes in the physiology and pathology of muscarinic signaling, and study of the structure of muscarinic receptors and structure-activation relationship of muscarinic ligands. Here we discuss the current state of knowledge of radioligand binding experiments at muscarinic receptors from the perspective of available radioligands and selective unlabeled muscarinic ligands. We relate binding properties of muscarinic ligands to experimental design (e.g., nonspecific binding determination, incubation conditions, buffers, temperature). We also list tissue/cell sources of muscarinic receptors suitable for radioligand binding studies and describe procedures of cell and tissue preparation for radioligand binding experiments. We also describe several techniques of receptor-bound ligand separation applicable at muscarinic receptors and provide basic information for binding data analysis.

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Acknowledgments

This research was supported by Academy of Sciences of the Czech Republic support RVO: 67985823, and Grant Agency of the Czech Republic grant P304/12/G069.

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Authors and Affiliations

  1. Department of Experimental and Clinical Pharmacology, University of Minnesota College of Pharmacy, 7-115 Weaver-Densford Hall, 308 Harvard St. SE, Minneapolis, MN, 55455, USA

    Esam E. El-Fakahany

  2. Institute of Physiology, Academy of Sciences of the Czech Republic, 14220, Prague, Czech Republic

    Jan Jakubik

Authors
  1. Esam E. El-Fakahany
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  2. Jan Jakubik
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Corresponding author

Correspondence to Esam E. El-Fakahany .

Editor information

Editors and Affiliations

  1. Institute of Physiology, Charles University, Prague, Czech Republic

    Jaromir Myslivecek

  2. Department of Neurochemistry, Acad. of Sciences of the Czech Rep. Institute of Physiology, Prague, Czech Republic

    Jan Jakubik

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El-Fakahany, E.E., Jakubik, J. (2016). Radioligand Binding at Muscarinic Receptors. In: Myslivecek, J., Jakubik, J. (eds) Muscarinic Receptor: From Structure to Animal Models. Neuromethods, vol 107. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2858-3_3

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  • DOI: https://doi.org/10.1007/978-1-4939-2858-3_3

  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-2857-6

  • Online ISBN: 978-1-4939-2858-3

  • eBook Packages: Springer Protocols

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