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Brain 5-HT2Creceptors: potential role in anxiety disorders

  • Chapter
Anxiolytics

Part of the book series: Milestones in Drug Therapy ((MDT))

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Abstract

Due to their predominant brain localization [1], 5HT2Creceptors offer innovative targets for designing novel psychotropic drugs for the treatment of psychiatric disorders. 5HT2Creceptors (formerly termed 5HTic) are members of the 5HT2receptor family [2-4] which also includes 5HT2Areceptors (formerly 5HT2receptors) and 5HT2Breceptors (formerly5HT2Freceptors). This G-protein coupled receptor family activates phospholipase C as a transduction mechanism. 5HT2receptor subtypes mutually share approximately 80% amino acid sequence homology but have distinct distributions in the body that suggest distinct physiological functions. Whereas 5HT2Areceptors are found in the brain and periphery, 5HT2Breceptors are mainly located in the periphery and 5HT2Creceptors are found only in the central nervous system (CNS), widely distributed throughout various brain regions [5]; in most brain areas binding sites, mRNA and immunolocalization of 5HT2Creceptors reveal a similar overall distribution [1, 6] and species differences between rat and human brain distribution are limited [7]. Their dense presence in limbic and cortical regions is consistent with a possible important role in affective disorders such as anxiety and/or depression. Lower density but significant functional coupling is found in the basal ganglia [8] while high 5HT2Creceptor density is found in the choroid plexus where its functional role remains to be elucidated. Neurotoxic lesion experiments indicate that 5HT2Creceptors are mostly post-synaptic but there is also evidence suggesting possible pre-synaptic localization on 5HT nerve terminals [9].

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Authors and Affiliations

  1. ROCHE Pharma Division, Preclinical CNS Research, CH-4070, Basel, Switzerland

    François Jenck, Jean-Luc Moreau, Jürgen Wichmann, Heinz Stadler & James R. Martin

  2. Boehringer Ingelheim, Virology Research Center, Montreal, Canada

    Michael Bös

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  3. Jürgen Wichmann
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  4. Heinz Stadler
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  5. James R. Martin
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  6. Michael Bös
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Editors and Affiliations

  1. Institut de Recherche Pierre Fabre, Parc Industriel de la Chartreuse, Castres, 81100, France

    Mike Briley

  2. Psychopharmacology Unit School of Medical Science, University of Bristol, University Walk, Bristol, BS8 1TD, UK

    David Nutt

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© 2000 Springer Basel AG

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Jenck, F., Moreau, JL., Wichmann, J., Stadler, H., Martin, J.R., Bös, M. (2000). Brain 5-HT2Creceptors: potential role in anxiety disorders. In: Briley, M., Nutt, D. (eds) Anxiolytics. Milestones in Drug Therapy. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-8470-9_9

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  • DOI: https://doi.org/10.1007/978-3-0348-8470-9_9

  • Publisher Name: Birkhäuser, Basel

  • Print ISBN: 978-3-0348-9581-1

  • Online ISBN: 978-3-0348-8470-9

  • eBook Packages: Springer Book Archive

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