Skip to main content
SpringerLink
Log in

Tricyclic antidepressants block histamine H1 receptors of mouse neuroblastoma cells

  • Letter
  • Published:

From Nature

View current issue Submit your manuscript

Abstract

TRICYCLIC antidepressants are structurally related to anti-histamines and are known to possess antihistaminic properties1. Green and co-workers2,24 showed that these drugs competitively antagonised histamine H2 receptor-mediated cyclic AMP formation by homogenates of guinea pig brain. Using muscarinic acetylcholine receptor-mediated cyclic GMP formation by mouse neuroblastoma cells (clone N1E-115)3, the interactions of psychotherapeutic drugs with this cholinergic receptor were studied in this laboratory4,5. While investigating the desensitisation of this muscarinic receptor6, it was found that histamine also stimulated cyclic GMP formation by activation of histamine H1 receptors of these cells7. This assay for histamine H1 receptors was used to obtain quantitative data for tricyclic antidepressant interactions with these receptors. This report shows that these drugs are potent competitive inhibitors of histamine H1 receptors and that some of these compounds are amongst the most potent H1 antagonists known.

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. Sigg, E. B. in Psychopharmacology A Review of Progress 1957–1967, (ed. Efron, D.) 662–663 (U.S. Public Health Service Publ. No. 1836, 1968).

    Google Scholar 

  2. Green, J. P. & Maayani, S. Nature 269, 163–165, (1977).

    Article  ADS  CAS  Google Scholar 

  3. Richelson, E. in International Review of Biochemistry, Ser. II, Physiological and Pharmacological Biochemistry (ed. Tipton, K.) (University Park Press, Baltimore, in the press).

  4. Richelson, E. Nature 266, 371–373 (1977).

    Article  ADS  CAS  Google Scholar 

  5. Richelson, E. & Divinetz-Romero, S. Biol. Psychiatr. 12, 771–785 (1977).

    CAS  Google Scholar 

  6. Richelson, E. Nature 272, 366–368 (1978).

    Article  ADS  CAS  Google Scholar 

  7. Richelson, E. Science (in the press).

  8. Richelson, E., Prendergast, F. G. & Divinetz-Romero, S. Biochem. Pharmac. (in the press).

  9. Waud, D. R. Pharmac. Rev. 20, 49–88 (1968).

    CAS  Google Scholar 

  10. Snyder, S. H. & Yamamura, H. I. Archs gen. Psychiat. 34, 236–239 (1977).

    Article  CAS  Google Scholar 

  11. Rehavi, M., Maayani, S. & Sokolovsky, M. Biochem. Pharmac. 26, 1559–1567 (1977).

    Article  CAS  Google Scholar 

  12. Hill, S. J., Young, J. M. & Marrian, D. H. Nature 270, 361–363 (1977).

    Article  ADS  CAS  Google Scholar 

  13. Marshall, P. B. Br. J. Pharmac. 10, 270–278 (1955).

    CAS  Google Scholar 

  14. U'Pritchard, D. C., Greenberg, D. A., Sheehan, P. P. & Snyder, S. H. Science 199, 197–198 (1978).

    Article  ADS  Google Scholar 

  15. Douglas, W. W. in The Pharmacological Basis of Therapeutics (eds. Goodman, L. S. & Oilman, A.) 603–611 (MacMillan, New York, 1975).

    Google Scholar 

  16. Hollister, L. E. Clinical Use of Psychotherapeutic Drugs (Charles C. Thomas, Springfield, 1973).

    Google Scholar 

  17. Jick, H. in Hypnotics (eds Kagan, F., Harwood, T., Richels, K., Rudzik, A. & Sores, H.) 145–154 (Spectrum, New York, 1975).

    Google Scholar 

  18. Davies, D. A. & Reid, J. L. (eds) Central Action of Drugs in Blood Pressure Regulation (University Park Press, Baltimore, 1975).

  19. Lorenz, W. et al. International Symposium on Histamine H2-Receptor Antagonists (eds Wood, C. J. & Simkins, M. A.) 151–165 (Smith, Kline and French Ltd, Welwyn Garden City, 1973).

    Google Scholar 

  20. Karppanen, H., Paakkari, I., Paakkari, P., Huatari, R. & Orma, A.-L. Nature 259, 587–588 (1976).

    Article  ADS  CAS  Google Scholar 

  21. Krishna, G., Weiss, B. & Brodie, B. B. J. Pharmac. exp. Ther. 163, 379–385 (1968).

    CAS  Google Scholar 

  22. Chan, P. S. & Lin, M. C. Meth. Enzym. 20, 38–41 (1974).

    Article  Google Scholar 

  23. Lowry, O., Rosebrough, N. J., Farr, L. & Randall, R. J. J. biol. Chem., 193, 265–275 (1951).

    CAS  Google Scholar 

  24. Maayani, S., Green, J. P. & Weinstein, H. Fedn Proc. 37, 612 (1978).

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Departments of Psychiatry and Pharmacology, Mayo Foundation, Rochester, Minnesota, 55901

    ELLIOTT RICHELSON

Authors
  1. ELLIOTT RICHELSON
    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

RICHELSON, E. Tricyclic antidepressants block histamine H1 receptors of mouse neuroblastoma cells. Nature 274, 176–177 (1978). https://doi.org/10.1038/274176a0

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1038/274176a0

  • Springer Nature Limited

This article is cited by

Search

Navigation