Skip to main content

The Benzodiazepine Receptor in Human Brain

  • Chapter
Sleep Research

Abstract

Benzodiazepines have found wide therapeutic application in the treatment of anxiety, sleep disorders, muscle spasms and convulsions. In the present report we describe recent progress in the clarification of the mechanism of action of benzodiazepines: benzodiazepines are bound to a specific target structure in the brain, termed benzodiazepine receptor, in order to elicit their pharmacological and therapeutic central effects. The receptor is characterized by a binding site highly specific for benzodiazepines. In addition to the identification, characteristics and distribution of the benzodiazepine receptor in normal human brain, its alteration in Huntington’s disease are described. Furthermore, present views on the biochemical mechanism of action of benzodiazepine are discussed.

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

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

Similar content being viewed by others

References

  1. Bird, E. D. and Iversen, L. L. (1974). Huntington’s chorea: postmortem measurement of glutamic acid decarboxylase, choline acetyltransferase and dopamine in basal ganglia. Brain, 97, 457–472

    Article  PubMed  CAS  Google Scholar 

  2. Braestrup, C., Nissen, C., Squires, R. F., Schousboe, A. (1970). Lack of brain specific benzodiazepine receptors on mouse primary astroglial cultures. Neurosa. Lett., 9, 45–49

    Article  Google Scholar 

  3. Braestrup, C. and Squires, R. F. (1977). Specific benzodiazepine receptors in rat brain characterized by high-affinity 3H-diazepam binding. Proc. Natl. Acad. Sci. USA, 74, 3805–3807

    Article  PubMed  CAS  Google Scholar 

  4. Braestrup, C., Albrechtsen, R. and Squires, R. F. (1977). High densities of benzodiazepine receptors in human cortical areas. Nature, 269, 702–704

    Article  PubMed  CAS  Google Scholar 

  5. Chang, R. S. L. and Snyder, S. H. (1978). Benzodiazepine receptors: labelling in intact animals with 3H-flunitrazepam. Eur. J. Pharmacol., 48, 213–218

    Article  PubMed  CAS  Google Scholar 

  6. Davies, J. and Pole, P. (1978). Effect of a water-soluble benzodiazepine on the responses of spinal neurones to acetylcholine and excitatory amino acid analogues. Neuropharmacology, 17, 217–220

    Article  PubMed  CAS  Google Scholar 

  7. Feldman, R. (1978). Discriminative properties of chlordiazepoxide: a new method of analysis. Psychopharmacology, 58 (2), p. 6, Abstr. No. 13

    Google Scholar 

  8. File, S. A. and Vellucci, S. V. (1978). Studies on the role of ACTH and 5-HT in anxiety, using an animal model. J. Pharm. Pharmacol., 30, 105–110

    Article  PubMed  CAS  Google Scholar 

  9. Gottschalk, L. A. and Elliott, A. W. (1976). Effects of triazolam and flurazepam on emotions and intellectual function. Res. Commun. Psychol., Psychiatr. Behav., 1, 575–595

    CAS  Google Scholar 

  10. Guidotti, A., Toffano, G. and Costa, E. (1978). An endogenous protein modulates the affinity of GABA and benzodiazepine receptors in rat brain. Nature, 275, 553–555

    Article  PubMed  CAS  Google Scholar 

  11. Haefely, W., Pole, P., Schaffner, R., Keller, H. H., Pieri, L. and Möhler, H. (1978). Facilitation of GABAergic transmission. In H. Kofod, P. Krogsgaard-Larsen and F. Scheel-Krüger (eds.), GABA Neurotransmitters. (In press)

    Google Scholar 

  12. Instructions for medical use provided by the manufacturers on the product information sheet of the commercially available drugs

    Google Scholar 

  13. Karobath, M. and Sperk, G. (1979). Stimulation of benzodiazepine receptor binding by γ-aminobutyric acid. Proc. Natl. Acad. Sci. USA. (In press)

    Google Scholar 

  14. Möhler, H. and Okada, T. (1977). Benzodiazepine receptor: demonstration in the central nervous system. Science, 198, 849–851

    Article  PubMed  Google Scholar 

  15. Möhler, H. and Okada, T. (1977). Properties of 3H-diazepam binding to benzodiazepine receptors in rat cerebral cortex. Life Sci., 20, 2101–2110

    Article  PubMed  Google Scholar 

  16. Möhler, H., Okada, T. and Bird, E. (1978). Huntington’s chorea: decrease in benzodiazepine-receptor binding. 7th Int. Congress of Pharmacology, Paris, Abstr. No. 2536

    Google Scholar 

  17. Möhler, H., Okada, T., Ulrich, J. and Heitz, Ph. (1978). Biochemical identification of the site of action of benzodiazepines in human brain by 3H-diazepam binding. Life Sci., 22, 985–996

    Article  PubMed  Google Scholar 

  18. Möhler, H., Pole, P., Cumin, R., Pieri, L. and Kettler, R. (1979). Nicotinamide or brain constituent with benzodiazepine-like action. Nature. (In press)

    Google Scholar 

  19. Nistri, A. and Constanti, A. (1978). Effects of flurazepam on amino acid evoked responses recorded from the lobster muscle and the frog spinal cord. Neuropharmacology, 17, 127–135

    Article  PubMed  CAS  Google Scholar 

  20. Okada, T., Spokes, E. G., Bird, E. D. and Möhler, H. (1979). Huntington’s chorea: decrease in benzodiazepine-receptor binding in putamen and caudate nucleus. (In preparation)

    Google Scholar 

  21. Okada, T. and Möhler, H. Ligand specificity of the brain benzodiazepine receptor. (In preparation)

    Google Scholar 

  22. Pegram, V., Robinson, C., Donaldson, P., Beaton, J. and Smythies, J. (1975). The effects of chronic use of nicotinamide on human sleep. 2nd Int. Congr. on Sleep Research, Edinburgh, Abstr., p. 91

    Google Scholar 

  23. Randall, L. O., Schallek, W., Sternbach, L. H. and Ning, R. Y. (1974). Chemistry and pharmacology of the 1,4-benzodiazepines. In M. Gordon (ed.), Psychopharmacological Agents, Vol. III, pp. 175–281

    Google Scholar 

  24. Robinson, C. R., Pegram, G. V., Hyde, P. R., Beaton, J. M. and Smythies, J. R. (1977). The effects of nicotinamide upon sleep in humans. Biol. Psychiatry, 12, 139–143

    PubMed  CAS  Google Scholar 

  25. Squires, R. F. and Braestrup, C. (1977). Benzodiazepine receptors in rat brain. Nature, 266, 732–734

    Article  PubMed  CAS  Google Scholar 

  26. Tallman, J. F., Thomas, J. W. and Gallager, D. W. (1978). GABAergic modulation of benzodiazepine binding site sensitivity. Nature, 274, 383–385

    Article  PubMed  CAS  Google Scholar 

  27. Toffano, G., Guidotti, A. and Costa, E. (1978). Purification of an endogenous protein inhibitor for the high-affinity binding of gamma-aminobutyric acid to synaptic membranes of rat brain. Proc. Natl. Acad. Sci. USA, 75, 4024–4028

    Article  PubMed  CAS  Google Scholar 

  28. Williamson, M. J., Paul, S. M. and Skolnick, P. (1978). Labelling of benzodiazepine receptors in vivo. Nature, 275, 551–553

    CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1979 MTP Press Limited

About this chapter

Cite this chapter

Möhler, H., Okada, T. (1979). The Benzodiazepine Receptor in Human Brain. In: Priest, R.G., Pletscher, A., Ward, J. (eds) Sleep Research. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-6226-5_1

Download citation

  • DOI: https://doi.org/10.1007/978-94-011-6226-5_1

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-011-6228-9

  • Online ISBN: 978-94-011-6226-5

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics