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

来源：

PSYCHOPHARMACOLOGY | 1997年 / 133卷 / 02期

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.

引用

页码：196 / 202

页数：7

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