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Titolo:
Evaluation of [4-O-methyl-C-11]KW-6002 as a potential PET ligand for mapping central adenosine A(2A) receptors in rats
Autore:
Hirani, E; Gillies, J; Karasawa, A; Shimada, J; Kase, H; Opacka-Juffry, J; Osman, S; Luthra, SK; Hume, SP; Brooks, DJ;
Indirizzi:
Hammersmith Hosp, Imaging Res Solut Ltd, London W12 0NN, England Hammersmith Hosp London England W12 0NN lut Ltd, London W12 0NN, England Hammersmith Hosp, PET Methodol Grp, MRC, Ctr Clin Sci, London W12 0NN, England Hammersmith Hosp London England W12 0NN lin Sci, London W12 0NN, England Kyowa Hakko Kogyo Co Ltd, Div Pharmaceut Res & Dev, Tokyo 1008185, Japan Kyowa Hakko Kogyo Co Ltd Tokyo Japan 1008185 & Dev, Tokyo 1008185, Japan Univ London Imperial Coll Sci Technol & Med, Sch Med, Div Neurosci, LondonW12 0NN, England Univ London Imperial Coll Sci Technol & Med London England W12 0NN gland
Titolo Testata:
SYNAPSE
fascicolo: 3, volume: 42, anno: 2001,
pagine: 164 - 176
SICI:
0887-4476(200112)42:3<164:EO[AAP>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON-EMISSION-TOMOGRAPHY; AGONIST H-3 CGS-21680; DOPAMINE INTERACTIONS; SELECTIVE LIGAND; BINDING-SITES; ANTAGONIST; BRAIN; KF17837; SYSTEM; AUTORADIOGRAPHY;
Keywords:
positron emission tomography; PET; rat brain; xanthine;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
45
Recensione:
Indirizzi per estratti:
Indirizzo: Hirani, E Hammersmith Hosp, Imaging Res Solut Ltd, MRC Cyclotron Bldg,Du Cane Rd, London W12 0NN, England Hammersmith Hosp MRC Cyclotron Bldg,Du CaneRd London England W12 0NN
Citazione:
E. Hirani et al., "Evaluation of [4-O-methyl-C-11]KW-6002 as a potential PET ligand for mapping central adenosine A(2A) receptors in rats", SYNAPSE, 42(3), 2001, pp. 164-176

Abstract

KW-6002, a xanthine-based adenosine A(2A) antagonist, was labelled with the positron emitter carbon-11 by O-methylation of its precursor, KF23325, using [C-11]iodomethane and was evaluated in rats as a putative in vivo radioligand for positron emission tomography (PET). Following intravenous injection of [C-11]KW-6002, radioactivity was measured in blood, plasma, peripheral tissues, and in discrete brain tissues over a 2-h time period commensurate with PET scanning, In brain, [C-11]KW-6002 showed highest retention in striata, with evidence of saturable binding, and lowest retention in frontalcortex (a tissue low in adenosine A(2A) receptors). PET scanning with [C-11]KW-6002 demonstrated a specific signal in the striata which could be described using compartmental modelling. Specific binding was, however, also detected in extrastriatal regions, including brain areas reported to have lowadenosine A(2A) receptor density. Blocking studies with the A(1) selectiveantagonist KF15372 and the non xanthine-type A2A antagonist ZM 241385 failed to elucidate the nature of this binding. Thus, although [C-11]KW-6002 shows some potential for development as a PET ligand for quantifying striataladenosine A(2A) receptor function, its in vivo selectivity requires further investigation. (C) 2001 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 21:31:45