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Does the tissue concentration in receptor binding studies change the affinity of the labelled ligand?

Authors
  • Ensing, K
  • De Zeeuw, R A
Type
Published Article
Journal
Pharmaceutisch weekblad. Scientific edition
Publication Date
Dec 14, 1984
Volume
6
Issue
6
Pages
241–244
Identifiers
PMID: 6514542
Source
Medline
License
Unknown

Abstract

When the tissue concentration in a radioreceptor assay for anticholinergic drugs was varied in order to obtain optimum conditions, and the receptor concentration Cr and the equilibrium dissociation constant KD were determined by Scatchard analysis, the KD increased with increasing tissue concentrations. This phenomenon was considered as an artefact caused by non-specific binding of the labelled ligand to constituents of the receptor preparation which were not completely retained on the glass-fibre filters used for the separation of bound and free fraction of radio-labelled ligand. The increase in KD in these experiments could be described with a mathematical model of the binding experiments.

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