5-HT2A Receptor Heterodimerization

  • Sylwia Łukasiewicz
  • Ewa Błasiak
  • Marta Dziedzicka-Wasylewska
Part of the The Receptors book series (REC, volume 32)


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.


Central serotonin 5-HT2A receptor G protein-coupled receptors (GPCRs) Heterodimerization Structural aspects Resonance energy transfer Psychotropic drugs 


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Copyright information

© Springer International Publishing AG 2018

Authors and Affiliations

  • Sylwia Łukasiewicz
    • 1
  • Ewa Błasiak
    • 1
  • Marta Dziedzicka-Wasylewska
    • 1
    • 2
  1. 1.Faculty of Biochemistry, Biophysics and BiotechnologyJagiellonian UniversityKrakówPoland
  2. 2.Institute of Pharmacology, Polish Academy of SciencesKrakówPoland

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