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Titolo:
Radiosynthesis of (+/-)-(2-((4-(2-[F-18]fluoroethoxy)phenyl)bis(4-methoxy-phenyl) methoxy)ethylpiperidine-3-carboxylic acid: a potential GAT-3 PET ligand to study GABAergic neuro-transmission in vivo
Autore:
Schirrmacher, R; Hamkens, W; Piel, M; Schmitt, U; Luddens, H; Hiemke, C; Rosch, F;
Indirizzi:
Inst Nucl Chem, D-55128 Mainz, Germany Inst Nucl Chem Mainz Germany D-55128 t Nucl Chem, D-55128 Mainz, Germany Univ Mainz, Dept Psychiat, D-6500 Mainz, Germany Univ Mainz Mainz Germany D-6500 nz, Dept Psychiat, D-6500 Mainz, Germany
Titolo Testata:
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
fascicolo: 9, volume: 44, anno: 2001,
pagine: 627 - 642
SICI:
0362-4803(200108)44:9<627:RO(>2.0.ZU;2-M
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; DOPAMINE TRANSPORTER; UPTAKE SITES; BRAIN; RADIOLIGAND; QUANTITATION; RADIOTRACER; RECEPTORS; AFFINITY;
Keywords:
GABA; GABA transporter ligand; [F-18]fluoroethyl-derivatives;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Rosch, F Inst Nucl Chem, D-55128 Mainz, Germany Inst Nucl Chem Mainz Germany D-55128 em, D-55128 Mainz, Germany
Citazione:
R. Schirrmacher et al., "Radiosynthesis of (+/-)-(2-((4-(2-[F-18]fluoroethoxy)phenyl)bis(4-methoxy-phenyl) methoxy)ethylpiperidine-3-carboxylic acid: a potential GAT-3 PET ligand to study GABAergic neuro-transmission in vivo", J LABEL C R, 44(9), 2001, pp. 627-642

Abstract

A dysfunction of GABAergic neurotransmission is related to diseases such as epilepsy, Huntington-disease and Parkinson-syndrome. A new F-18-fluorine labelled GABA transporter ligand for the GABA-transporter subtype GAT-3 wasdeveloped which may allow the in vivo visualisation of GABAergic neurotransmission. The precursors ethyl (2-(4-hydroxyphenyl)bis (4-methoxyphenyl)-methoxy)ethyl)-piperidine-3-carboxylate and ethyl(2-((4(2-tosylethoxy)phenyl)-bis(4-methoxyphenyl)-methoxy) ethyl)piperidine-3-carboxylate were synthesised and labelled by the use of 2-[F-18]fluoroethyltosylate or [18F]fluoride, Subsequent cleavage of the ester moiety gave the final product (+/-)-(2-((4-(2-[F-18]fluoroethoxy)phenyl) bis(4-methoxy-phenyl)methoxy)ethyl)piperidine-3-carboxylic acid in a decay corrected yield of 33-36%. Preliminary biodistribution kinetics were determined with BALB/c mice ex vivo for brain., liver, kidney. spleen, blood and bone. (2-((4-(2-[F-18]fluoroethoxy)-phenyl)bis(4-methoxyphenyl)methoxy)-ethyl) piperidine-3-carboxylic acid showed a maximum brain uptake after 1 h p.i. of about 0.3% ID/g. Copyright (C) 2001 John Wiley & Sons, Ltd.

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Documento generato il 22/01/20 alle ore 06:48:47