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Titolo:
EVALUATION OF THE BINDING OF THE RADIOLABELED ANTIDEPRESSANT DRUG, F-18 FLUOXETINE IN THE RODENT BRAIN - AN IN-VITRO AND IN-VIVO STUDY
Autore:
MUKHERJEE J; DAS MK; YANG ZY; LEW R;
Indirizzi:
KETTERING MED CTR,DEPT NUCL MED PET,3535 SO BLVD KETTERING OH 45429 UNIV CHICAGO,FRANKLIN MCLEAN INST,DEPT RADIOL CHICAGO IL 60637 UNIV CHICAGO,FRANKLIN MCLEAN INST,DEPT PHARMACOL & PHYSIOL SCI CHICAGO IL 60637
Titolo Testata:
Nuclear medicine and biology
fascicolo: 7, volume: 25, anno: 1998,
pagine: 605 - 610
SICI:
0969-8051(1998)25:7<605:EOTBOT>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN-UPTAKE INHIBITOR; FLUOXETINE PROZAC; REUPTAKE SITES; C-11; RAT; PET; NORFLUOXETINE; RADIOTRACER;
Keywords:
F-18 FLUOXETINE (F-18-PROZAC); AUTORADIOGRAPHY; SEROTONIN TRANSPORTER; MONOAMINE OXIDASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
J. Mukherjee et al., "EVALUATION OF THE BINDING OF THE RADIOLABELED ANTIDEPRESSANT DRUG, F-18 FLUOXETINE IN THE RODENT BRAIN - AN IN-VITRO AND IN-VIVO STUDY", Nuclear medicine and biology, 25(7), 1998, pp. 605-610

Abstract

We have developed F-18-fluoxetine as a radiotracer analog of the antidepressant drug fluoxetine (Prozac), In vitro saturation experiments of F-18-fluoxetine were carried out on rat midbrain tissue and citalopram was used for measuring nonspecific binding. A saturation curve for the binding of F-18-fluoxetine was not obtained. Even when fluoxetine (10 mu M) was used for measurements of nonspecific binding, a saturation curve was difficult to obtain. Other compounds, such as deprenyl, clorgyline, amphetamine, and reserpine were also not able to reduce thebinding of F-18-fluoxetine. Ex vivo autoradiographic experiments withF-18-fluoxetine did not reveal any specific uptake in various brain regions. In vivo administration of 18F-fluoxetine in rats showed similar uptake in all the brain regions with little regional selectivity. A subcellular analysis of rat brain tissue after intravenous (IV) administration of F-18 fluoxetine indicated significant amounts of binding in mitochondria and synaptosomes, In summary, in vitro experiments withF-18-fluoxetine indicate little specific binding. Binding to the serotonin transporter was not identifiable. High nonspecific binding of the tracer resulting from its subcellular nature in the brain masks the ability to detect binding to the serotonin uptake sites in vivo. Thesefindings indicate that a large portion of the binding of F-18-fluoxetine in rat brains is subcellular and clears slowly out of the cells, Other sites, such as monoamine oxidase, may also play a significant role in the action of fluoxetine. (C) 1998 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/06/20 alle ore 09:34:31