Agents and Actions

, Volume 18, Issue 1–2, pp 231–234 | Cite as

Histamine H2-binding on guinea pig cerebral cortex

  • G. J. Sterk
  • M. W. G. van der Schaar
  • B. Rademaker
  • H. van der Goot
  • H. Timmerman
Histamine and Central Nervous System

Abstract

The Kd-values of some histamine H2-active compounds, obtained from radio-ligand-binding studies on a homogenate of the guinea-pig cerebral cortex with3H-tiotidine as the labelled H2-ligand, were compared with the pA2/pD2-value of these compounds on the guinea-pig right atrium and guinea-pig isolated gastric fundus. A good correlation was found between the pKd of the H2-antagonists and their pA2 on the guinea-pig right atrium. A much poorer correlation however was obtained between the pKd of the agonists on the cerebral cortex and their pD2-values on the guinea-pig right atrium and the gastric fundus. This poor correlation between true affinity and H2-activity of the agonists might be explained by spare receptors as a much better correlation was obtained between pKd and pD2 of partial agonists.

Keywords

Histamine Cerebral Cortex Poor Correlation Partial Agonist Gastric Fundus 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. [1]
    T.J. Rising, D.B. Norris, S.E. Warrander andT.P. Wood,High affinity 3 H-cimetidine binding in guinea-pig tissues, Life Sci.27, 199–206 (1980).CrossRefPubMedGoogle Scholar
  2. [2]
    I.R. Smith, M.T. Cleverley, C.R. Ganellin andK.M. Metters,Binding of [3 H]cimetidine to rat brain tissue, Agents Actions10, 422–426 (1980).PubMedGoogle Scholar
  3. [3]
    G.A. Gajtkowski, D.B. Norris, T.J. Rising andT.P. Wood,Specific binding of 3 H-tiotidine to histamine H 2-receptors in guinea pig cerebral cortex, Nature304, 65–67 (1983).CrossRefPubMedGoogle Scholar
  4. [4]
    G.J. Sterk, H. van der Goot andH. Timmerman,Studies on histaminergic compounds. Part II — synthesis and histamine H 2-activity of dimaprit and some of its analogues, Eur. J. Med. Chem. — Chim. Ther.19, 545–550 (1984).Google Scholar
  5. [5]
    M. Impicciatore, G. Morini andG. Bertaccini,The effects of stimulants and inhibitors of histamine receptors on acid secretion from guinea-pig gastric fundus, Eur. J. Pharmacol.48, 249–254 (1978).CrossRefPubMedGoogle Scholar
  6. [6]
    P.J. Munson andD. Rodboard,LIGAND: A versatile computarized approach for characterization of ligand-binding systems, Anal. Biochem.107, 220–239 (1980).PubMedGoogle Scholar
  7. [7]
    K.M. Verburg andD.P. Henry,Binding of histamine by glass surfaces, Agents Actions14, 633–636 (1984).PubMedGoogle Scholar

Copyright information

© Birkhäuser Verlag 1986

Authors and Affiliations

  • G. J. Sterk
    • 1
  • M. W. G. van der Schaar
    • 1
  • B. Rademaker
    • 1
  • H. van der Goot
    • 1
  • H. Timmerman
    • 1
  1. 1.Department of PharmacochemistryVrije UniversiteitAmsterdamThe Netherlands

Personalised recommendations