Skip to main content

Receptor binding methods: application to the study of cyclopyrrolones, a new family of minor tranquillizers

  • Chapter
Veterinary Pharmacology and Toxicology

Abstract

The receptor theory is not a new one. It was first introduced at the beginning of this century between 1905 and 1910 by Ehrlich working on tetanus toxin and trypanocidal dyes and Langley working on the action of nicotine and curare on muscle16. At that time, of course, very limited proof supported this notion which was almost purely conceptuall. However, many pharmacological studies thereafter, especially those of Clark around 1926, reinforced the interest in this concept which became very fruitful and was finally validated during the 1960s when the existence of receptors was directly established, thanks to the development of binding techniques with radio-labelled ligands1. A new and decisive stage was reached with the isolation around 1977 of the nicotinic receptor from the electric organ of electric fishes11.

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 139.00
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 179.99
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.

References

  1. Ariens, E. J. (1979). Receptors: from fiction to fact. T.I.P.S.,1, 11–15

    CAS  Google Scholar 

  2. Bardone, M. C., Ducrot, R., Garret, C. et al. (1978). Benzodiazepine-like central effects of RP 27 267, a dihydro-7-oxo-5 H-pyrrolo [3, 4-b] pyrazine derivative. Presented at7th International Congress of Pharmacology, Paris. Abstract 2319

    Google Scholar 

  3. Blanchard, J. C., Boireau, A., Garret, C. et al. (1979). In vitro and in vivo inhibition by zopiclone of benzodiazepine binding to rodent brain receptors.Life Sci,24, 2417–20

    Article  CAS  PubMed  Google Scholar 

  4. Blanchard, J. C. and Julou, L. (1983). Suriclone: a new cyclopyrrolone derivative recognizing receptors labelled by benzodiazepines in rat hippocampus and cerebellum.J. Neurochem,50, 601–7

    Article  Google Scholar 

  5. Blanchard, J. C., Boireau, A. and Julou, L. (1982). Brain receptors and zopiclone. Presented at13th C.I.N.P. Congress, Jerusalem. Abst. p. 799

    Google Scholar 

  6. Braestrup, C., Albrechtsen, R. and Squires, R. F. (1977). High densities of benzodiazepine receptors in human cortical areas.Nature (London),263, 702–4

    Article  Google Scholar 

  7. Burch, T. P. and Ticku, M. K. (1981). Histidine modification with diethylpyrocarbonate shows heterogeneity of benzodiazepine receptors.Proc. Natl. Acad. Sci,78, 3945–9

    Article  CAS  PubMed  Google Scholar 

  8. Cuatrecasas, P., Hollenberg, M. D., Chang, K.-J. et al. (1975). Hormone receptor complexes and their modulation of membrane function.Rec. Prog. Horm. Res,31, 37–84

    CAS  PubMed  Google Scholar 

  9. Gallager, D. W., Mallorga, P., Thomas, J. W. et al. (1980). GABA-benzodiazepine interactions: physiological, pharmacological and developmental aspects.Fed. Proc,39, 3043–9

    CAS  PubMed  Google Scholar 

  10. Garret, C., Bardone, M. C., Blanchard, J. C. et al. (1982). Pharmacological studies of suriclone (RP 31 264) a cyclopyrrolone derivative with anxiolytic properties. Presented at13th C.I.N.P. Congress, Jerusalem. Abst. p. 244

    Google Scholar 

  11. Heidmann, T. and Changeux, J. P. (1978). Structural and functional properties of the acetylcholine receptor protein in its purified and membrane bound states.Ann. Rev. Biochem,47, 317–57

    Article  CAS  PubMed  Google Scholar 

  12. Marangos, P. J., Paul, S. M. and Goodwin, F. K. (1979). Putative endogenous ligands for the benzodiazepine receptor.Life Sci,25, 1093–102

    Article  CAS  PubMed  Google Scholar 

  13. Möhler, H. and Okada, T. (1977). Benzodiazepine receptor: demonstration in the central nervous system.Science,198, 849–51

    Article  PubMed  Google Scholar 

  14. Möhler, H. and Okada, T. (1978). Biochemical identification site of action of benzodiazepines in human brain by 3H diazepam binding.Life Sci, 22, 985–96

    Article  PubMed  Google Scholar 

  15. Olsen, R. W. (1981). GABA-benzodiazepine-barbiturate receptor interactions.Neurochem,37, 1–13

    Article  CAS  Google Scholar 

  16. Parascandola, J. (1980). Origins of the receptor theory.T.I.P.S,1, 189–92

    CAS  Google Scholar 

  17. Sherman-Gold, R. and Dudai, Y. (1981). Involvement of tyrosyl residues in the binding of benzodiazepines to their brain receptor.FEBS Letters,131, 313–6

    Article  CAS  PubMed  Google Scholar 

  18. Snyder, S. H. (1978). Overview of neurotransmitter receptor binding. In Neurotransmitter Receptor Binding, pp. 1 - 11. ( New York: Raven Press )

    Google Scholar 

  19. Squires, R. F. and Braestrup, C. (1977). Benzodiazepine receptors in rat brain.Nature (London),266, 732 - 4

    Article  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1983 MTP Press Limited

About this chapter

Cite this chapter

Blanchard, J.C., Julou, L. (1983). Receptor binding methods: application to the study of cyclopyrrolones, a new family of minor tranquillizers. In: Ruckebusch, Y., Toutain, PL., Koritz, G.D. (eds) Veterinary Pharmacology and Toxicology. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-6604-8_44

Download citation

  • DOI: https://doi.org/10.1007/978-94-009-6604-8_44

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-009-6606-2

  • Online ISBN: 978-94-009-6604-8

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics