PET-characterization of [carbonyl-C-11]WAY-100635 binding to 5-HT1A receptors in the primate brain
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Farde, L
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
Farde, L
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Ginovart, N
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
Ginovart, N
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Ito, H
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
Ito, H
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Lundkvist, C
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
Lundkvist, C
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Pike, VW
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
Pike, VW
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McCarron, JA
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
McCarron, JA
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Halldin, C
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HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLANDHAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
Halldin, C
[1
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[1] HAMMERSMITH HOSP, ROYAL POSTGRAD MED SCH, CHEM & ENGN CYCLOTRON UNIT, LONDON W12 0HS, ENGLAND
[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.