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

被引:64
作者
Farde, L [1 ]
Ginovart, N [1 ]
Ito, H [1 ]
Lundkvist, C [1 ]
Pike, VW [1 ]
McCarron, JA [1 ]
Halldin, C [1 ]
机构
[1] HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
关键词
5-HT1A-receptors; positron emission tomography; monkey brain; carbonyl-C-11]WAY-100635; 8-OH-DPAT; buspirone; pindolol;
D O I
10.1007/s002130050391
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
[carbonyl-C-11]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-C-11]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-C-11]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-C-11]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:7
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