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Titolo:
In vitro and in vivo evaluation of the binding of the dopamine D2 receptoragonist C-11-(R,S)-5-hydroxy-2-(di-n-propylamino)tetralin in rodents and nonhuman primate
Autore:
Mukherjee, J; Narayanan, TK; Christian, BT; Shi, BZ; Dunigan, KA; Mantil, J;
Indirizzi:
Wright State Univ, Kettering Med Ctr, Dept Internal Med Nucl Med, Dayton, OH 45435 USA Wright State Univ Dayton OH USA 45435 Med Nucl Med, Dayton, OH 45435 USA
Titolo Testata:
SYNAPSE
fascicolo: 1, volume: 37, anno: 2000,
pagine: 64 - 70
SICI:
0887-4476(200007)37:1<64:IVAIVE>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
INVIVO DISTRIBUTION; ANTERIOR-PITUITARY; HIGH-AFFINITY; GUANINE-NUCLEOTIDE; RAT-BRAIN; STATE; 2-AMINOTETRALINS;
Keywords:
C-11-5-OH-DPAT; dopamine D2 receptor agonist; in vitro autoradiography; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Mukherjee, J Kettering Med Ctr, Dept Nucl Med PET, 3535 So Blvd, Dayton, OH 45429 USA Kettering Med Ctr 3535 So Blvd Dayton OH USA 45429 45429 USA
Citazione:
J. Mukherjee et al., "In vitro and in vivo evaluation of the binding of the dopamine D2 receptoragonist C-11-(R,S)-5-hydroxy-2-(di-n-propylamino)tetralin in rodents and nonhuman primate", SYNAPSE, 37(1), 2000, pp. 64-70

Abstract

The in vitro autoradiographic binding characteristics as well as in vivo imaging characteristics of a dopamine D2 receptor agonist, (R, S)-2-(N-propyl-N-1'-C-11-propyl)amina-5-hydroxytetralin (C-11-5-OH-DPAT), were studied. In H-3-spiperone assays using rat striata, 5-OH-DPAT exhibited an affinity of IC50 = 2.5 nM. In vitro autoradiographs in rat brain slices with C-11-5-OH-DPAT revealed selective binding to the dopaminergic regions in the striata which was displaceable by sulpiride. Varying concentrations of dopamine displaced this selective binding of C-11-5-OH-DPAT to the striata in rat brain slices. This selective binding to the striata was also removed in the presence of the GTP analog, 5'-guanylylimidodiphosphate, indicative of the binding of C-11-5-OH-DPAT to the high-affinity state of the D2 receptor. Ex vivo autoradiographic study in rats exhibited selective binding of C-11-5-OH-DPAT to the striata. A PET study in a rhesus monkey showed selective localization of C-11-5-OH-DPAT in the striata and the ratio between striata andcerebellum approached approximately 2 at 40 min postinjection. (C) 2000 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 10:17:01