Encyclopedia of Psychopharmacology

2015 Edition
| Editors: Ian P. Stolerman, Lawrence H. Price

Receptors: Functional Assays

Reference work entry
DOI: https://doi.org/10.1007/978-3-642-36172-2_208


Measurement of biological effect resulting from interaction with the receptor; Measurement of receptor signaling


Psychoactive drugs generally exert their effects by binding to a specific recognition site, whether that is associated with a receptor, a transporter, or an enzyme, and thereby alter the function of that receptor, enzyme, or transporter. However, receptors are the predominant targets for psychoactive drugs (Grigoriadis et al. 2009), and these may be either G-protein-coupled receptors (GPCRs) or, to a lesser extent, ion channels (the latter being either ligand or voltage gated).

Although the actual effect produced by drugs affecting GPCRs and ion channels is very different, their mechanisms of action follow similar principles. Hence, a drug acting at a GPCR or ion channel may block the effect of an endogenous agonist (i.e., acts as an antagonist), mimic the effect of the endogenous activator (i.e., acts as an agonist), or inhibit spontaneous...

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© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  1. 1.Janssen Research and DevelopmentA Division of Janssen PharmaceuticaBeerseBelgium
  2. 2.Translational Drug Discovery Group, School of Life SciencesUniversity of SussexBeerseBelgium