Skip to main content
SpringerLink
Log in

Binding of [3H]cimetidine to rat brain tissue

  • Histamine and Kinins
  • Published:
Agents and Actions Aims and scope Submit manuscript

Abstract

Binding of [3H]cimetidine to rat brain tissue was investigated, and a saturable binding with dissociation constant 0.22±0.05 μM found. This binding is inhibited by a range of imidazole-derived histamine H2-receptor antagonists, but not by a number of non-imidazole H2-receptor antagonists. It is concluded that the [3H]cimetidine binding site in rat brain tissue that is labelled in these experiments is not the histamine H2-receptor.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. M. Chasin, F. Mamrak, S.G. Samaniego andS.M. Hess,Characteristics of the Catecholamine and Histamine Receptor sites Mediating Accumulation of Cyclic Adenosiee 3′,5′-Monophosphate in Guinea-Pig Brain, J. Neurochem.21, 1415 (1973).

    PubMed  Google Scholar 

  2. K. Dismukes, M. Rogers andJ.W. Daly,Cyclic Adenosine 3′,5′-Monophosphate Formation in Guinea-Pig Brain Slices: Effect of H 1 -and H 2 -Histaminergic Agonists, J. Neurochem.26, 785 (1976).

    PubMed  Google Scholar 

  3. J.M. Palacios, M. Garbarg, G. Barbin andJ.C. Schwartz,Pharmacological Characterization of Histamine Receptors Mediating the Stimulation of Cyclic AMP Accumulation in Slices from Guinea-Pig Hippocampus, Mol. Pharmacol.14, 971 (1978).

    PubMed  Google Scholar 

  4. J.P. Green, C.L. Johnson, H. Weinstein andS. Maayani,Antagonism of Histamine-Activated Adenylate Cyclase in Brain by D-Lysergic Acid Diethylamide, Proc. nat. Acad. Sci USA74, 5697 (1977).

    PubMed  Google Scholar 

  5. P.D. Kanof andP. Greengard,Pharmacological Properties of Histamine-Sensitive Adenylate Cyclase from Mammalian Brain, J. Pharmac. exp. Ther.209, 87 (1979).

    Google Scholar 

  6. S.R. Nahorski, K.J. Rogers andB.M. Smith,Stimulation of Cyclic Adenosine 3′,5′-monophosphate in Chick Cerebral Hemisphere Slices: Effects of H 1 and H 2 Histaminergic Agonists and Antagonists, Brain Res.126, 387 (1977).

    Article  PubMed  Google Scholar 

  7. S.J. Hill, P.C. Emson andJ.M. Young,The Binding of [3H]mepyramine to Histamine H 1 -Receptors in Guinea Pig Brain, J. Neurochem.31, 997 (1978).

    Google Scholar 

  8. R.S.L. Chang, V.T. Tran andS.H. Snyder,Heterogeneity of Histamine H 1 -Receptors: Species Variations in [3 H]mepyramine Binding of Brain Membranes, J. Neurochem.32, 1653 (1979).

    Google Scholar 

  9. V.T. Tran, R.S.L. Chang andS.H. Synder,Histamine H 1 -Receptors Identified in Mammalian Brain Membranes with [3 H]mepyramine, Proc. nat. Acad. Sci. USA75, 6209 (1978).

    Google Scholar 

  10. M. Rehavt andM. Sokolovsky,Multiple Binding Sites of Tricyclic Antidepressant Drugs to Mammalian Brain Receptors, Brain Res.149, 525 (1978).

    Article  PubMed  Google Scholar 

  11. W.P. Burkard,Histamine H 2 -Receptor Binding with [3 H]metidine in Brain, Eur. J. Pharmac.50, 449 (1978).

    Article  Google Scholar 

  12. D.A. Kendall, J.W. Ferkany andS.J. Enna,Properties of [3 H]cimetidine Binding in Rat Brain Membrane Fractions, Life Sciences26, 1293 (1980).

    Article  PubMed  Google Scholar 

  13. G.N. Wilkinson,Statistical Estimations in Enzyme Kinetics, Biochem. J.80, 324 (1961).

    PubMed  Google Scholar 

  14. R.J. Lefkowitz, L.E. Limbird, C. Mukherjee andM.G. Caron,The β-Adrenergic Receptor and Adenylate Cyclase, Biochim. Biophys. Acta457, 1 (1976).

    PubMed  Google Scholar 

  15. T.O. Yellin, S.H. Buck, D.J. Gilman, D.F. Jones andJ.M. Wardleworth,ICI 125, 211: a Potent New Antisecretory Drug Acting on Histamine H 2 -Receptors, The Pharmacologist21, 266 (1979), Abstract 635.

    Google Scholar 

  16. J. Bradshaw, R.T. Brittain, J.W. Clitherow, M.J. Daly, D. Jack, B.J. Price andR. Stables,Ranitidine (AH 19065): a New Potent, Selective Histamine H 2 -Receptor Antagonist, Br. J. Pharmac.66, 464P (1979).

  17. J.P. Green andS. Maayani,Tricyclic Antidepressant Drugs Block Histamine H 2 -Receptor in Brain, Nature, Lond.269, 163 (1977).

    Google Scholar 

  18. P.D. Kanof andP. Greengard,Brain Histamine Receptors as Targets for Antidepressant Drugs, Nature, Lond.,272, 329 (1978).

    Google Scholar 

  19. M.E. Parsons, D.A.A. Owen, C.R. Ganellin andG.J. Durant,Dimaprit-[S-]3(N,N-dimethylamino)-propylisothiourea] — A Highly Specific Histamine H 2 -Receptor Agonist,Agents and Actions7, 31 (1977).

    PubMed  Google Scholar 

  20. G.J. Durant, W.A.M. Duncan, C.R. Ganellin, M.E. Parsons, R.C. Blakemore andA.C. Rasmussen,Impromidine (SK&F 92676) is a very Potent and Specific Agonist for Histamine H 2 -Receptors, Nature, Lond.276, 403 (1978).

    Google Scholar 

  21. S.T. Nielsen, T.O. Yellin, P.N. Edwards andM.S. Large,Radioligand Binding Assay of H 2 -Receptors with [3 H]ICIA 5165, The Pharmacologist21, 265 (1979), Abstract 634.

    Google Scholar 

  22. C.R. Ganellin,Selectivity and the Design of Histamine H 2 -Receptor Antagonists, J. appl. Chem. Biotechnol.28, 183 (1978).

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Research Institute, Smith Kline and French Research Ltd., AL7 1EY, Welwyn Garden City, Herts, UK

    Ian R. Smith, Mark T. Cleverley, C. Robin Ganellin & Kathleen M. Metters

Authors
  1. Ian R. Smith
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Mark T. Cleverley
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. C. Robin Ganellin
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Kathleen M. Metters
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Smith, I.R., Cleverley, M.T., Robin Ganellin, C. et al. Binding of [3H]cimetidine to rat brain tissue. Agents and Actions 10, 422–426 (1980). https://doi.org/10.1007/BF01968040

Download citation

  • Received:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF01968040

Keywords

Search

Navigation