Related Experiment Video
Updated: Aug 10, 2026

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis
Published on: July 3, 2015
Cation dependence of opioid receptor binding supports theory on membrane-mediated receptor selectivity
D F Sargent1, J W Bean, H W Kosterlitz
1Department of Molecular Biology and Biophysics, Swiss Federal Institute of Technology, Zürich.
Abstract:
A quantitative analysis of the binding of dynorphin A-(1-9)-nonapeptide to the opioid Kappa-receptors of the guinea pig cerebellum [Paterson et al. (1986) Proc. Natl. Acad. Sci. U.S.A. 83, 6216-6220] shows that changes in electrostatic surface accumulation of the ligand fully account for the observed suppression of binding by a series of univalent and divalent salts. Binding to mu- and delta-receptors, on the other hand, is subject to additional ion-specific effects. These observations support the membrane locations for the receptor sites proposed by the "membrane compartments" theory for opioid receptor selection.
Related Concept Videos
Drug-Receptor Bonds
In...
Drug-Receptor Interactions
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
Quantitative Aspects of Drug-Receptor Interaction
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...
Opioid Receptors: Overview
Analgesia and Pain Management

