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5-HT2A Receptors in the Central Nervous System pp 57–66Cite as

5-HT2A Receptor Heterodimerization

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Part of the book series: The Receptors ((REC,volume 32))

Abstract

Interaction of serotonin 5-HT2A receptor with other G protein-coupled receptors (GPCRs) have been shown at the behavioral and/or electrophysiological level. In the present chapter evidence for direct physical interactions of this receptor with various GPCRs have been described. The most interesting in the context of antipsychotic drug action mechanism is the interaction of the serotonin 5-HT2A receptor with dopamine D2 receptor, which has been shown both in vitro as well as in the native brain tissue. On the other hand, new understanding of hallucinogenic drugs has been proposed by providing data which demonstrate the formation of heterocomplexes by the 5-HT2A receptor with the metabotropic glutamatergic receptor mGluR2. Methodology used in GPCRs heterodimerization studies has evolved, from radioligand binding, receptor crosslinking, receptor complementation, or co-immunoprecipitation approach to biophysical techniques based on resonance energy transfer—each having their pros and cons, however their use still provides new exciting data concerning the complexity of GPCRs physical interactions, which broaden basal knowledge as well as offer new targets for pharmacological intervention.

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Authors and Affiliations

  1. Faculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Kraków, Poland

    Sylwia Łukasiewicz, Ewa Błasiak & Marta Dziedzicka-Wasylewska

  2. Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland

    Marta Dziedzicka-Wasylewska

Authors
  1. Sylwia Łukasiewicz
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  2. Ewa Błasiak
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  3. Marta Dziedzicka-Wasylewska
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Correspondence to Marta Dziedzicka-Wasylewska .

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Editors and Affiliations

  1. Faculté de Pharmacie, Université Paris Sud, Université Paris-Saclay, Chatenay-Malabry, France

    Bruno P. Guiard

  2. Department of Physiology and Biochemistry, University of Malta, Msida MSD, Malta

    Giuseppe Di Giovanni

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Łukasiewicz, S., Błasiak, E., Dziedzicka-Wasylewska, M. (2018). 5-HT2A Receptor Heterodimerization. In: Guiard, B., Di Giovanni, G. (eds) 5-HT2A Receptors in the Central Nervous System. The Receptors, vol 32. Humana Press, Cham. https://doi.org/10.1007/978-3-319-70474-6_3

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