Affordable Access

Publisher Website

High affinity binding of tricyclic antidepressants to histamine H1-receptors: Fact and artifact

Authors
Journal
European Journal of Pharmacology
0014-2999
Publisher
Elsevier
Publication Date
Volume
67
Issue
1
Identifiers
DOI: 10.1016/0014-2999(80)90006-0
Keywords
  • Tricyclic Antidepressants
  • Histamine H1-Receptor
Disciplines
  • Biology

Abstract

Abstract Six tricyclic antidepressants were tested for their ability to inhibit the binding of the histamine H 1-receptor antagonist [ 3H]pyrilamine to membrane fractions from whole rat brain. Calculated inhibition constants (K i) for the antidepressants were in the range of 2.6 × 10 −11 to 2.3 × 10 −7M and correlated very well with their equilibrium dissociation constants derived from biological assays of the H 1-receptor. Increasing the concentration of receptors present in the binding assay resulted in an overestimation of the calculated K i's for doxepin, amitriptyline, and nortriptyline, but not for the lower affinity compounds of the series, imipramine, protriptyline, and desipramine. These results indicate: (1) the importance of receptor concentration in determining the potency of compounds which competitively inhibit, with very high affinity, the binding of a radioactively labeled ligand; (2) the need to correlate binding data with biological data.

There are no comments yet on this publication. Be the first to share your thoughts.

Statistics

Seen <100 times
0 Comments

More articles like this

High affinity binding of tricyclic antidepressants...

on European Journal of Pharmacolo... Oct 03, 1980

High-affinity binding of mequitamium iodide (LG 30...

on European Journal of Pharmacolo... Jan 01, 1990

Tricyclic antidepressants: Potent blockade of hist...

on European Journal of Pharmacolo... Jan 01, 1979

Tricyclic antidepressants and histamine H1 recepto...

on Mayo Clinic Proceedings October 1979
More articles like this..