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Titolo:
Synthesis and preliminary evaluation of a carbon-11-labeled adenosine transporter blocker [C-11]KF21652
Autore:
Ishiwata, K; Takai, H; Nonaka, H; Ishii, S; Simada, J; Senda, M;
Indirizzi:
Tokyo Metropolitan Inst Gerontol, Positron Med Ctr, Tokyo 1730022, Japan Tokyo Metropolitan Inst Gerontol Tokyo Japan 1730022 okyo 1730022, Japan Kyowa Hakko Kogyo, Pharmaceut Res Inst, Drug Discovery Res Labs, Nagaizumi, Shizuoka 4118731, Japan Kyowa Hakko Kogyo Nagaizumi Shizuoka Japan 4118731 hizuoka 4118731, Japan
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 3, volume: 28, anno: 2001,
pagine: 281 - 285
SICI:
0969-8051(200104)28:3<281:SAPEOA>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
A(2A) RECEPTOR-LIGAND; NITROBENZYLTHIOINOSINE BINDING; UPTAKE SITE; BRAIN; AUTORADIOGRAPHY; LOCALIZATION; KF15372; KF18446; KF17837; VIVO;
Keywords:
adenosine transporter blocker; [C-11]KF21652; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Ishiwata, K Tokyo Metropolitan Inst Gerontol, Positron Med Ctr, 1-1 Naka-cho, Tokyo 1730022, Japan Tokyo Metropolitan Inst Gerontol 1-1 Naka-cho Tokyo Japan 1730022
Citazione:
K. Ishiwata et al., "Synthesis and preliminary evaluation of a carbon-11-labeled adenosine transporter blocker [C-11]KF21652", NUCL MED BI, 28(3), 2001, pp. 281-285

Abstract

We prepared an C-11-labeled adenosine transporter blocker, [1-methyl-C-11]-3-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H, 3H)-quinazolinedione ([C-11]KF21652) and examined its potential as a positronemission tomography (PET) ligand for mapping adenosine transporters in thebrain and peripheral organs. The log P-7,P-4 value of KF21652 was 3.14, and the K-i value was 13 nM for adenosine transporters using [H-3]nitrobenzylthioinosine as a radioligand. In mice, the highest initial uptake was foundin the liver, followed by the kidney and small intestine. The brain uptakewas very low. The radioactivity level slightly increased with time in the liver and small intestine, but decreased in the other organs. Coinjection of carrier KF21652 slightly decreased the uptake of [C-11]KF21562 only in the liver, but not in any other organs. Ex vivo autoradiography of the rat brain showed that [C-11]KF21652 was scarcely incorporated into the brain. On the other hand, in vitro autoradiography showed the binding of [C-11]KF21562 to adenosine transporters with high nonspecific binding. These results show that the compound is not a suitable PET ligand for mapping adenosine transporters. (C) 2001 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 07:26:20