Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Tumor Necrosis Factor-α Mediates Inflammation-induced Early-Stage Left Ventricular Systolic Dysfunction.

Journal of cardiovascular pharmacology·2023
Same author

Increased protein phosphatase 5 expression in inflammation-induced left ventricular dysfunction in rats.

BMC cardiovascular disorders·2022
Same author

Inflammation-induced left ventricular fibrosis is partially mediated by tumor necrosis factor-α.

Physiological reports·2021
Same author

Similarities and differences in the reproductive phenotypes of women with congenital hypogonadotrophic hypogonadism caused by GNRHR mutations and women with polycystic ovary syndrome.

Human reproduction (Oxford, England)·2018
Same author

Glu<sup>2.53(90)</sup> of the GnRH receptor is part of the conserved G protein-coupled receptor structure and does not form a salt-bridge with Lys<sup>3.32(121)</sup>.

Molecular and cellular endocrinology·2018
Same author

Gonadotropin-Releasing Hormone (GnRH) Receptor Structure and GnRH Binding.

Frontiers in endocrinology·2017

Related Experiment Video

Updated: Mar 24, 2026

Monitoring GPCR-&#946;-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
08:21

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

7.5K

GPCR-radioligand binding assays.

Colleen A Flanagan1

  • 1School of Physiology and Medical Research Council Receptor Biology Research Unit, Faculty of Health Sciences, University of the Witwatersrand, Wits Parktown, Johannesburg, South Africa.

Methods in Cell Biology
|March 2, 2016
PubMed
Summary

Radioligand binding assays are crucial for studying G protein-coupled receptors (GPCRs) and drug development. These methods quantify receptor expression and ligand affinity, aiding structure-activity relationship studies.

Keywords:
Binding equilibriumIndirect bindingLigand depletionRadioligand bindingRadioligand binding artifactsSaturation binding

More Related Videos

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

15.9K
Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

17.4K

Related Experiment Videos

Last Updated: Mar 24, 2026

Monitoring GPCR-&#946;-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
08:21

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

7.5K
Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

15.9K
Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

17.4K

Area of Science:

  • Pharmacology
  • Biochemistry
  • Molecular Biology

Background:

  • G protein-coupled receptors (GPCRs) are vital drug targets.
  • Radioligand binding assays are essential for GPCR research and drug discovery.
  • Understanding ligand-receptor interactions is key for developing new therapeutics.

Purpose of the Study:

  • To outline fundamental radioligand binding assay protocols.
  • To detail the assessment of GPCR expression and ligand affinity.
  • To explain the determination of binding parameters and interaction mechanisms.

Main Methods:

  • Saturation binding assays to determine receptor density (Bmax).
  • Indirect (competition/displacement) assays for ligand affinity (Ki).
  • Kinetic assays to measure association and dissociation rates.

Main Results:

  • Accurate measurement of GPCR expression and ligand binding affinity.
  • Distinguishing between competitive and allosteric ligand binding mechanisms.
  • Identification of factors affecting assay accuracy, such as radioligand depletion and equilibration time.

Conclusions:

  • Radioligand binding assays are indispensable tools for GPCR research.
  • Optimization of assay conditions is critical for reliable data.
  • These assays facilitate drug structure-activity relationship studies and basic GPCR science.