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

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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.

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Authors and Affiliations

  1. Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, S-171 76 Stockholm, Sweden Fax (+8) 346563, e-mail: lars.fard.@neuro.ks.se, , , , , , SE

    L. Farde, Nathalie Ginovart, Hiroshi Ito, Camilla Lundkvist & Christer Halldin

  2. Chemistry and Engineering Cyclotron Unit, Royal Postgraduate Medical School, Hammersmith Hospital, Ducan Road, London W12 0HS, UK, , , , , , GB

    Victor W. Pike & Julie A. McCarron

Authors
  1. L. Farde
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  2. Nathalie Ginovart
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  3. Hiroshi Ito
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  4. Camilla Lundkvist
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  5. Victor W. Pike
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  6. Julie A. McCarron
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  7. Christer Halldin
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Received: 24 December 1996/Final version: 7 March 1997

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Farde, L., Ginovart, N., Ito, H. et al. PET-characterization of [carbonyl-11C]WAY-100635 binding to 5-HT1A receptors in the primate brain. Psychopharmacology 133, 196–202 (1997). https://doi.org/10.1007/s002130050391

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  • DOI: https://doi.org/10.1007/s002130050391

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