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Titolo:
In vitro and in vivo characterisation of [H-3]ANSTO-14 binding to the sigma(1) binding sites
Autore:
Nguyen, VH; Mardon, K; Kassiou, M; Christie, MJ;
Indirizzi:
Australian,Nucl Sci & Technol Org, Radiopharmaceut R&D Div, Menai, NSW 2234 Australian Nucl Sci & Technol Org Menai NSW Australia 2234 enai, NSW 2234 Univ Sydney, Dept Pharmacol, Sydney, NSW 2006, Australia Univ Sydney Sydney NSW Australia 2006 rmacol, Sydney, NSW 2006, Australia Royal Prince Alfred Hosp, Dept Pet & Nucl Med, Camperdown, NSW, Australia Royal Prince Alfred Hosp Camperdown NSW Australia erdown, NSW, Australia
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 2, volume: 26, anno: 1999,
pagine: 209 - 215
SICI:
0969-8051(199902)26:2<209:IVAIVC>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; CENTRAL NERVOUS-SYSTEM; LIGAND-BINDING; RECEPTOR; RAT; 1-PHENYL-3-AMINO-1,2,3,4-TETRAHYDRONAPHTHALENES; PHENYLAMINOTETRALINS; TRISHOMOCUBANES; RADIOLIGAND; ANTAGONISTS;
Keywords:
sigma; binding sites; trishomocubanes; biodistribution; metabolite; ANSTO-14;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Nguyen, VH AustraliangNucl Sci & Technol Org, Radiopharmaceut R&D Div, Private Mail Ba Australian Nucl Sci & Technol Org Private Mail Bag 1 Menai NSWAustralia 2234
Citazione:
V.H. Nguyen et al., "In vitro and in vivo characterisation of [H-3]ANSTO-14 binding to the sigma(1) binding sites", NUCL MED BI, 26(2), 1999, pp. 209-215

Abstract

N-(4-phenylbutyl)-3-hydroxy-4-azahexacyclo[5.4.1.0(2.6).0(3.10).0(5,9).0(8.11)]dodecane (ANSTO-14) showed the highest activity for the sigma(1) site (K-i = 9.4 nM) and 19-fold sigma(1)/sigma(2) selectivity. The present studyshowed that [H-3]ANSTO-14 binds to a single high-affinity site in guinea pig brain membranes with an equilibrium K-d of 8.0 +/- 0.3 nM, in good agreement with the kinetic studies (K-d = 13.3 +/- 5.4 nM, n = 4), and a B-max of 3,199 +/- 105 fmol/mg protein (n = 4). The in vivo biodistribution of [H-3]ANSTO-14 showed a high uptake in the diencephalon. Pretreatment of rats with sigma ligands including (+)-pentazocine (sigma(1)), ANSTO-14 (sigma(1)), and DTG (sigma(1) and sigma(2)) did not significantly reduce radiotracer uptake in the brain, but did in the spleen. A labelled metabolite was foundin the liver and brain. Due to its insensitivity to a ligands, the accumulation of [H-3]ANSTO-14 in the brain indicates high nonspecific binding. Therefore, [H-3]ANSTO-14 is a suitable ligand for labelling sigma(1) sites in vitro but is not suitable for brain imaging of sigma binding sites In vivo. NUCL MED BIOL 26;2:209-215, 1999. (C) 1999 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/06/20 alle ore 11:17:51