Psychopharmacology

, Volume 133, Issue 2, pp 196–202

PET-characterization of [carbonyl-11C]WAY-100635 binding to 5-HT1A receptors in the primate brain

Authors

  • L. Farde
    • Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, S-171 76 Stockholm, Sweden Fax (+8) 346563, e-mail: lars.fard.@neuro.ks.se
  • Nathalie Ginovart
    • Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, S-171 76 Stockholm, Sweden Fax (+8) 346563, e-mail: lars.fard.@neuro.ks.se
  • Hiroshi Ito
    • Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, S-171 76 Stockholm, Sweden Fax (+8) 346563, e-mail: lars.fard.@neuro.ks.se
  • Camilla Lundkvist
    • Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, S-171 76 Stockholm, Sweden Fax (+8) 346563, e-mail: lars.fard.@neuro.ks.se
  • Victor W. Pike
    • Chemistry and Engineering Cyclotron Unit, Royal Postgraduate Medical School, Hammersmith Hospital, Ducan Road, London W12 0HS, UK
  • Julie A. McCarron
    • Chemistry and Engineering Cyclotron Unit, Royal Postgraduate Medical School, Hammersmith Hospital, Ducan Road, London W12 0HS, UK
  • Christer Halldin
    • Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, S-171 76 Stockholm, Sweden Fax (+8) 346563, e-mail: lars.fard.@neuro.ks.se
ORIGINAL INVESTIGATION

DOI: 10.1007/s002130050391

Cite this article as:
Farde, L., Ginovart, N., Ito, H. et al. Psychopharmacology (1997) 133: 196. doi:10.1007/s002130050391

Abstract

[carbonyl- 11C]WAY-100635 is a new radioligand which can be used with positron emission tomography (PET) to provide high contrast delineation of human brain regions that are rich in 5-HT1A receptors. In the present PET study, the binding of [carbonyl- 11C]WAY-100635 was characterized in the cynomolgus monkey brain. Pretreatment with each of the two reference compounds, WAY-100635 and 8-OH-DPAT, as well as the drugs buspirone and pindolol, induced a marked inhibition of [carbonyl-11C]WAY-100635 binding in the neocortex and the raphe nuclei. A preliminary Scatchard analysis yielded 5-HT1A receptor density values of the same order as those that have been reported in vitro. The study shows that [carbonyl- 11C]WAY-100635 binds specifically to 5-HT1A receptors in the primate brain and has potential for determination of 5-HT1A receptor occupancy and density in psychiatric patients.

Key words 5-HT1A-receptors Positron emission tomography Monkey brain [Carbonyl-11C]WAY-100635 8-OH-DPAT Buspirone Pindolol

Copyright information

© Springer-Verlag Berlin Heidelberg 1997