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The 5-HT1A receptor and its ligands: structure and function

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Progress in Drug Research

Part of the book series: Progress in Drug Research ((PDR,volume 52))

Summary

An overview is presented on progress made in research on 5-HT1A receptors and their ligands since their discovery in 1983. Molecular biology has offered new tools, for example cloned 5-HT1A receptors, their mutants and chimeras to study structure and function. Many compounds, belonging to different chemical classes, display high affinity and selectivity for 5-HT1A receptors. The majority of these compounds are agonists or partial agonists, full antagonists are still scarce. Agonists and partial agonists are active in various animal models of anxiety and depression. Partial receptor agonists have been proven to be effective in general anxiety disorder and depression in man. Potential therapeutic applications for 5-HT1A receptor antagonists are evaluated, for example, in cognition disorders.

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Abbreviations

5-HT:

5-hydroxytryptamine (serotonin)

8-OH-DPAT:

8-hydroxy-2-(di-n-propylamino)tetralin

SSRI:

selective serotonin reuptake inhibitors

5-HTT:

5-HT transporter

TM:

transmembrane domain

IA:

intrinsic activity

DRL 72 s:

differential reinforcement of low rates – 72 seconds.

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Authors and Affiliations

  1. Dept. of Psychopharmacology, Utrecht University, Sorbonnelaan 16, NL-3584, CA Utrecht, Netherlands

    Berend Olivier (Faculty of Pharmacy)

  2. CNS-Research, Solvay Pharmaceuticals B.V., P.O.Box 900, NL-1380, DA, Weesp, The Netherlands

    Berend Olivier (Faculty of Pharmacy)

  3. Leiden/Amsterdam Center for Drug Research, P.O. Box 9502, NL-2300, RA Leiden, The Netherlands

    Willem Soudijn & Ineke van Wijngaarden

Authors
  1. Berend Olivier
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  2. Willem Soudijn
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  3. Ineke van Wijngaarden
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Editor information

Editors and Affiliations

  1. Steinweg 28, CH-4107, Ettingen, Switzerland

    Ernst Jucker

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© 1999 Springer Basel AG

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Olivier, B., Soudijn, W., van Wijngaarden, I. (1999). The 5-HT1A receptor and its ligands: structure and function. In: Jucker, E. (eds) Progress in Drug Research. Progress in Drug Research, vol 52. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-8730-4_3

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  • DOI: https://doi.org/10.1007/978-3-0348-8730-4_3

  • Publisher Name: Birkhäuser, Basel

  • Print ISBN: 978-3-0348-9746-4

  • Online ISBN: 978-3-0348-8730-4

  • eBook Packages: Springer Book Archive

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