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

被引：0
|
作者：
L. Farde
Nathalie Ginovart
Hiroshi Ito
Camilla Lundkvist
Victor W. Pike
Julie A. McCarron
Christer Halldin
机构：
[1] Psychiatry Section,
[2] Department of Clinical Neuroscience,undefined
[3] Karolinska Institutet,undefined
[4] S-171 76 Stockholm,undefined
[5] Sweden Fax (+8) 346563,undefined
[6] e-mail: lars.fard.@neuro.ks.se,undefined
[7] Chemistry and Engineering Cyclotron Unit,undefined
[8] Royal Postgraduate Medical School,undefined
[9] Hammersmith Hospital,undefined
[10] Ducan Road,undefined
[11] London W12 0HS,undefined
[12] UK,undefined
来源：
Psychopharmacology | 1997年 / 133卷
关键词：
Key words 5-HT1A-receptors; Positron emission tomography; Monkey brain; [Carbonyl-11C]WAY-100635; 8-OH-DPAT; Buspirone; Pindolol;
D O I：
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中图分类号：
学科分类号：
摘要：
[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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页码：196 / 202
页数：6
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