Skip to main content

Selective Agonists and Antagonists at 5-Hydroxytryptamine Receptor Subtypes

  • Chapter
Serotonin

Abstract

In the late forties and early fifties 5-hydroxytryptamine (serotonin, 5-HT) was a fashionable research area, but thereafter activity declined and the field remained dormant for almost 20 years. During the past decade there has been renewed and steadily increasing interest, largely due to the availability of many new compounds with claimed selectivity for 5-HT receptor subtypes. Whilst some of them indeed show true selectivity, the majority of these compounds have appreciable affinity either for more than one 5-HT receptor subtype, or for other neurotransmitter receptors, and this limits their usefulness. Here we provide an update on the pharmacological properties of some of the more commonly used agonists and antagonists at 5-HT receptors, in an attempt to identify those compounds, or combinations of compounds, which can be reliably used for the characterization of 5-HT receptors.

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 259.00
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 329.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 329.99
Price excludes VAT (USA)
  • Durable hardcover 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. Bradley, P.B., Engel, G., Feniuk, W., Fozard, J.R., Humphrey, P.P.A., Middlemiss, D.N., Mylecharane, E.J., Richardson, B.P. and Saxena, P.R. (1986). Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine. Neuropharmacology 25, 563–576.

    Article  PubMed  CAS  Google Scholar 

  2. Bradley, P.B., Engel, G., Feniuk, W., Fozard, J.R., Humphrey, P.P.A., Middlemiss, D.N., Mylecharane, E.J., Richardson, B.P. and Saxena, P.R. (1986). Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine. Neuropharmacology 25, 563–576.

    Article  PubMed  CAS  Google Scholar 

  3. Schoeffter, P. and Hoyer, D. (1988). Centrally acting hypotensive agents with affinity to 5-HT binding sites inhibit forskolin-stimulated adenylate cyclase in calf hippocampus. Br. J. Pharmacol. 95, 975–985.

    Google Scholar 

  4. Bouhelal, R., Smounya, L. and Bockaert, J. (1988). 5-HT1B receptors are negatively coupled with adenylate cyclase in rat substantia nigra. Eur. J. Pharmacol. 151, 189–196.

    Google Scholar 

  5. Schoeffter, P. Waeber, C., Palacios, J.M. and Hoyer, D. (1988). The serotonin 5-HT1D receptor subtype is negatively coupled to adenylate cyclase in calf substantia nigra. Naunyn Schmiedeberg’s Arch. Pharmacol. 337, 602–608.

    Google Scholar 

  6. Hoyer, D., Waeber, C., Schoeffter, P., Palacios, J.M. and Dravid, A. (1989). 5-HTlc-receptor mediated stimulation of inositol phosphate production in pig choroid plexus. Naunyn Schmiedebergs’s Arch. Pharmacol. 339, 252–258.

    Google Scholar 

  7. Hoyer, D., Engel, G. and Kalkman, H.O. (1985)., Molecular pharmacology of 5-HT1and 5-HT2 recognition sites in rat and pig brain membranes: radioligand binding studies with [3H] 5-HT, [3H]8-OH-DPAT, (-) [125I] iodocyanopindolol, [3H] mesulergine and [3H] ketanserin. Eur. J. Pharmcol. 118, 13–23.

    Google Scholar 

  8. Doyle, V.M., Creba, J.A., Rtiegg, U.T. and Hoyer, D. (1986). Serotonin increases the production of inositol phosphate and mobilizes calcium via the 5-HT2 receptor in A7r5 smooth muscle cells. Naunyn Schmieberg’s Arch. Pharmcol. 333, 98-103.

    Google Scholar 

  9. Richardson, B.P. and Buchheit, K-H. (1988) ‘The Pharmacology distribution and function of 5-HT 3 receptors’, in N.N. Osborne and M. Hamon (eds.). Neuronal Serotonin. John Wiley and Sons Ltd. Chichester, New York, Brisbane, Toronto, Singapore, pp. 465–506.

    Google Scholar 

  10. Conn, J.P., Sanders-Bush, E., Hoffman, B.J. and Hartig, P.R. (1986). A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol hydrolysis. Proc. Natl. Acad. Sci. USA, 83, 4086–4088.

    Google Scholar 

  11. Glennon, R.A. (1987). Central serotonin receptors as targets for drug research. J. Med. Chem. 30, 1–12.

    Google Scholar 

  12. Glennon, R.A. (1987). Central serotonin receptors as targets for drug research. J. Med. Chem. 30, 1–12.

    Article  PubMed  CAS  Google Scholar 

  13. Ireland, S.J. and Tyers, M.B. (1987). Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve. Br. J. Pharmacol. 90, 229–238.

    Google Scholar 

  14. Sanger, G.J. (1987). Increased gut cholinergic activity and antagonism of 5-hydroxytryptamine M-receptors BRL 24924: potential clinical importance of BRL 24924. Br. J. Pharmacol. 91, 77–87.

    Google Scholar 

  15. Dumuis, A., Sebben, M. and Bockaert, J. (1989). BRL 24924: A potent agonist at 5-HT1 receptors positively coupled with adenylate cyclase in colliculi neurones. Eur. J. Pharmacol. 162, 381–384.

    Google Scholar 

  16. Craig, D.A. and Clarke, D.E. (1989). 5-Hydroxytryptamine and cholinergic mechanisms in guinea pig ileum. Brit. J. Pharmacol. 96, 247P.

    Google Scholar 

  17. Hartig, P.R. (1989). Molecular biology of 5-HT receptors. Trends in Pharmacol. Sci. 10, 64–69.

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1990 Kluwer Academic Publishers

About this chapter

Cite this chapter

Richardson, B.P., Hoyer, D. (1990). Selective Agonists and Antagonists at 5-Hydroxytryptamine Receptor Subtypes. In: Paoletti, R., Vanhoutte, P.M., Brunello, N., Maggi, F.M. (eds) Serotonin. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-1912-9_34

Download citation

  • DOI: https://doi.org/10.1007/978-94-009-1912-9_34

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-7353-0

  • Online ISBN: 978-94-009-1912-9

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics