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Titolo:
Preliminary assessment of extrastriatal dopamine D-2 receptor binding in the rodent and nonhuman primate brains using the high affinity radioligand, F-18-fallypride
Autore:
Mukherjee, J; Yang, ZY; Brown, T; Lew, R; Wernick, M; Ouyang, XH; Yasillo, N; Chen, CT; Mintzer, R; Cooper, M;
Indirizzi:
Univ Chicago, Franklin Mclean Mem Res Inst, Dept Radiol, Chicago, IL 60637USA Univ Chicago Chicago IL USA 60637 Inst, Dept Radiol, Chicago, IL 60637USA Univ Chicago, Franklin Mclean Mem Res Inst, Dept Pharmacol & Physiol Sci, Chicago, IL 60637 USA Univ Chicago Chicago IL USA 60637 ol & Physiol Sci, Chicago, IL 60637 USA IIT, Dept Elect & Comp Engn, Chicago, IL 60616 USA IIT Chicago IL USA 60616 T, Dept Elect & Comp Engn, Chicago, IL 60616 USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 5, volume: 26, anno: 1999,
pagine: 519 - 527
SICI:
0969-8051(199907)26:5<519:PAOEDD>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN; AUTORADIOGRAPHIC LOCALIZATION; I-125 EPIDEPRIDE; PHARMACOLOGICAL CHARACTERIZATION; D-2-DOPAMINE RECEPTORS; PET; VISUALIZATION; NEUROLEPTICS; CLOZAPINE; SUBTYPES;
Keywords:
extrastriatal dopamine D-2 receptors; F-18-fallypride; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
30
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., "Preliminary assessment of extrastriatal dopamine D-2 receptor binding in the rodent and nonhuman primate brains using the high affinity radioligand, F-18-fallypride", NUCL MED BI, 26(5), 1999, pp. 519-527

Abstract

We have identified the value of F-18-fallypride ((S)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-[F-18]fluoropropyl)-2,3-dimethoxybenzamide as a dopamineD-2 receptor radiotracer for the study of striatal and extrastriatal receptors. Fallypride exhibits high affinities for D-2 and D-3 subtypes and low affinity for D-4 (H-3-spiperone IC(50)s: D-2 = 0.05 nM [rat striata], D-3 =0.30 nM [SF9 cell lines, rat recombinant], and D-4 = 240 nM [CHO cell lines, human recombinant]). Biodistribution in the rat brain showed localization of F-18-fallypride in striata and extrastriatal regions such as the frontal cortex, parietal cortex, amygdala, hippocampus, thalamus, and hypothalamus. In vitro autoradiographic studies in sagittal slices of the rat brain showed localization of F-18-fallypride in striatal and several extrastriatalregions, including the medulla. Positron emission tomography (PET) experiments with F-18-fallypride in male rhesus monkeys were carried out in a PET VI scanner. In several PET experiments, apart from the specific binding seen in the striatum, specific binding of F-18-fallypride was also identified in extracellular regions tin a lower brain slice, possibly the thalamus). Specific binding in the extrastriata was, however, significantly lower compared with that observed in the striata of the monkeys (extrastriata/cerebellum = 2, striata/cerebellum = 10). Postmortem analysis of the monkey brain revealed significant F-18-fallypride binding in the striata, whereas bindingwas also observed in extrastriatal regions such as the thalamus, cortical areas, and brain stem. (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 20/11/19 alle ore 02:42:18