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Technologies for Screening of mGlu Receptor Allosteric Modulators

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Metabotropic Glutamate Receptor Technologies

Part of the book series: Neuromethods ((NM,volume 164))

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Abstract

In recent years, modulation of metabotropic glutamate (mGlu) receptors has been explored in efforts for development of therapeutics, particularly for central nervous system disorders. Positive and negative allosteric modulators can engender compounds with the ability to selectively modulate mGlu receptor signaling pathways with therapeutically beneficial results. There are many assays available for the screening and characterization of mGlu receptor modulators, but a number of considerations should be addressed when selecting the appropriate assay. These can include mode of pharmacology, desired throughput, methodology for monitoring receptor activity, and assay kinetics. In this chapter, we discuss assays currently being used to identify and characterize allosteric modulators of mGlu receptors, highlight examples in the literature of these assays being successfully implemented, and provide detailed methods for executing these assays in the laboratory.

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Acknowledgments

The authors acknowledge support from rettsyndrome.org, Autism Speaks, NIMH R21 MH102548, R01 MH113543, and CDMRP grant W81XWH-17-1-0266.

Author information

Authors and Affiliations

  1. Department of Pharmacology and Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN, USA

    Alice L. Rodriguez & Colleen M. Niswender

  2. Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Nashville, TN, USA

    Colleen M. Niswender

Authors
  1. Alice L. Rodriguez
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  2. Colleen M. Niswender
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Corresponding author

Correspondence to Colleen M. Niswender .

Editor information

Editors and Affiliations

  1. Psychology Department, Arizona State University, Tempe, AZ, USA

    M Foster Olive

  2. Phoenix Children’s Hospital, Barrow Neurological Institute, Phoenix, AZ, USA

    Brian T. Burrows

  3. Psychology Department, Arizona State University, Tempe, AZ, USA

    Jonna M. Leyrer-Jackson

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Rodriguez, A.L., Niswender, C.M. (2021). Technologies for Screening of mGlu Receptor Allosteric Modulators. In: Olive, M.F., Burrows, B.T., Leyrer-Jackson, J.M. (eds) Metabotropic Glutamate Receptor Technologies. Neuromethods, vol 164. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1107-4_1

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  • DOI: https://doi.org/10.1007/978-1-0716-1107-4_1

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  • Publisher Name: Humana, New York, NY

  • Print ISBN: 978-1-0716-1106-7

  • Online ISBN: 978-1-0716-1107-4

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