PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635

被引：60

作者：

Carson, RE ^{[1
]}

Lan, LX ^{[1
]}

Watabe, H ^{[1
]}

Der, MG ^{[1
]}

Adams, HR ^{[1
]}

Jagoda, E ^{[1
]}

Herscovitch, P ^{[1
]}

Eckelman, WC ^{[1
]}

机构：

[1] NIH, Warren Grant Magnuson Clin Ctr, PET Dept, Bethesda, MD 20892 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 05期

关键词：

FCWAY; 5-HT1A receptors; modeling; volume of distribution;

D O I：

10.1016/S0969-8051(00)00118-9

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

We synthesized [F-18]FCWAY, an analog of [carbonyl-C-11]WAY-100635 ([C-11]N-(2-(1-(4(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridinyl))cyclohexanecarboxamide}, by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [F-18]FC and [F-18]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [F-18]FCWAY has very similar kinetic characteristics to [C-11]WAY-100635. NUCL MED BIOL 27;5:493-497, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：493 / 497

页数：5

共 50 条

[11] FIRST DELINEATION OF 5-HT1A RECEPTOR IN HUMAN BRAIN WITH PET AND [C-11]WAY-100635
PIKE, VW
MCCARRON, JA
LAMMERSTMA, AA
HUME, SP
POOLE, K
GRASBY, PM
MALIZIA, A
CLIFFE, IA
FLETCHER, A
BENCH, C
EUROPEAN JOURNAL OF PHARMACOLOGY, 1995, 283 (1-3) : R1 - R3
[12] A 5-HT-evoked depolarisation is revealed by the 5-HT1A antagonist way-100635 in the rat DRN.
Robinson, SM
Larkman, PM
Kelly, JS
EUROPEAN JOURNAL OF NEUROSCIENCE, 1998, 10 : 348 - 348
[13] Synthesis of a [6-pyridinyl-18F]-labelled fluoro derivative of WAY-100635 as a candidate radioligand for brain 5-HT1A receptor imaging with PET
Karramkam, M
Hinnen, F
Berrehouma, M
Hlavacek, C
Vaufrey, F
Halldin, C
McCarron, JA
Pike, VW
Dollé, F
BIOORGANIC & MEDICINAL CHEMISTRY, 2003, 11 (13) : 2769 - 2782
[14] Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist
Fletcher, A
Forster, EA
Bill, DJ
Brown, G
Cliffe, IA
Hartley, JE
Jones, DE
McLenachan, A
Stanhope, KJ
Critchley, DJP
Childs, KJ
Middlefell, VC
Lanfumey, L
Corradetti, R
Laporte, AM
Gozlan, H
Hamon, M
Dourish, CT
BEHAVIOURAL BRAIN RESEARCH, 1996, 73 (1-2) : 337 - 353
[15] [F-18]fluoroalkyl analogues of the potent 5-HT1A antagonist WAY 100635: Radiosyntheses and in vivo evaluation
Wilson, AA
DaSilva, JN
Houle, S
NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (04): : 487 - 490
[16] QUANTITATIVE AUTORADIOGRAPHIC CHARACTERIZATION OF THE BINDING OF [H-3] WAY-100635, A SELECTIVE 5-HT1A RECEPTOR ANTAGONIST
KHAWAJA, X
BRAIN RESEARCH, 1995, 673 (02) : 217 - 225
[17] 5-HT1A receptor imaging in the human brain using [C-11]WAY-100635 and PET.
Ito, H
Halldin, C
Lundkvist, C
Swahn, CG
Pike, V
Farde, L
JOURNAL OF NUCLEAR MEDICINE, 1997, 38 (05) : 1202 - 1202
[18] Tracer kinetic modeling of the 5-HT1A receptor ligand [carbonyl-11C]WAY-100635 for PET
Gunn, RN
Sargent, PA
Bench, CJ
Rabiner, EA
Osman, S
Pike, VW
Hume, SP
Grasby, PM
Lammertsma, AA
NEUROIMAGE, 1998, 8 (04) : 426 - 440
[19] Fluoroalkyl Derivatives of the 5-HT1A Antagonist WAY 100635
Wilson, A. A.
DaSilva, J. N.
Houle, S.
Journal of Labelled Compounds and Radiopharmaceuticals,
[20] EVALUATION OF [18F]FPWAY AND [18F]FBWAY, 5-HT1A RECEPTOR PET LIGANDS, FOR SENSITIVITY TO ENDOGENOUS 5-HT IN RAT
Jagoda, E. M.
Lang, L.
Tokugawa, J.
Ma, Y.
Contoreggi, C.
Eckelman, W. C.
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2005, 48 : S74 - S74

← 1 2 3 4 5 →