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Titolo:
Effects of dopamine on the in vivo binding of dopamine D-2 receptor radioligands in rat striatum
Autore:
Moresco, RM; Loch, C; Ottaviani, M; Guibert, B; Leviel, V; Maziere, M; Fazio, F; Maziere, B;
Indirizzi:
Univ Milan, Dept Nucl Med, Sci Inst H San Raffaele, CNR,INB, I-20132 Milan, Univ Milan Milan Italy I-20132 t H San Raffaele, CNR,INB, I-20132 Milan, CEA, Serv Hosp Frederic Joliot, DRM, F-91406 Orsay, France CEA Orsay France F-91406 osp Frederic Joliot, DRM, F-91406 Orsay, France CNRS, Inst Alfred Fessard, F-91198 Gif Sur Yvette, France CNRS Gif Sur Yvette France F-91198 ssard, F-91198 Gif Sur Yvette, France
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 1, volume: 26, anno: 1999,
pagine: 91 - 98
SICI:
0969-8051(199901)26:1<91:EODOTI>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; EARLY PARKINSONS-DISEASE; ENDOGENOUS DOPAMINE; C-11 RACLOPRIDE; D2 RECEPTOR; HUMAN-BRAIN; N-METHYLSPIPERONE; H-3 RACLOPRIDE; RELEASED DOPAMINE; INVIVO BINDING;
Keywords:
dopamine receptors; emission tomography; raclopride; NCQ298; iodolisuride;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
51
Recensione:
Indirizzi per estratti:
Indirizzo: Moresco, RM Univ60,lan, Dept Nucl Med, Sci Inst H San Raffaele, CNR,INB, Via Olgettina Univ Milan Via Olgettina 60 Milan Italy I-20132 Via Olgettina
Citazione:
R.M. Moresco et al., "Effects of dopamine on the in vivo binding of dopamine D-2 receptor radioligands in rat striatum", NUCL MED BI, 26(1), 1999, pp. 91-98

Abstract

The effects of moderate changes in extracellular dopamine concentrations on the in vivo binding of specific dopaminergic D-2 radioligands with different affinities and kinetics were investigated in rats. Either [I-125]NCQ298(Kd = 19 pM), or [I-125]iodolisuride (Kd = 0.27 nM) or [H-3]raclopride (Kd= 1.5 nM) were administered intravenously (IV) to animals 1 h after the intraperitoneal (IP) injection of either alpha-methyl-p-tyrosine (AMPT) (250 mg/kg) or nomifensine (15 mg/kg), or saline. The kinetics of radioactivity concentration in the striatum, cerebellum, and plasma were measured for up to 4 h after [I-125]NCQ298 or [I-125]iodolisuride injection and up to 1.5 hafter [H-3]raclopride injection. For each tracer, the striatum-to- cerebellum radioactivity concentration ratios (S/C) and the binding potential (BP), calculated as the association to dissociation binding rate constant ratios (k3/k4), were assessed and related to the changes in extracellular dopamine concentration induced by drug treatments. Results show that S/C and BP of [H-3]raclopride were significantly diminished by pretreatment with nomifensine, a drug that increases extracellular dopamine concentration. Nomifensine pretreatment induced no changes in the in vivo binding indexes of the high affinity [I-125]NCQ298 and a slight but not significant decrease of thebinding indexes of [I-125]iodolisuride. Treatment with AMPT, which induceda 40% reduction in dopamine concentration, did not change [I-125]NCQ298 binding indexes but slightly increased those of [H-3]raclopride and [I-125]iodolisuride. In conclusion, the change of dopamine concentration induces modification of radiotracer kinetics. Thus, the combined use of tracers with high and low affinities could allow us to obtain information both on receptor density and neurotransmitter release in vivo. However, as indicated by the [H-3]raclopride study with AMPT, small changes in the concentration of intrasynaptic dopamine cannot be easily detected. NUCL MED BIOL 26;1:91-98, 1999. (C) 1998 Elsevier Science Inc.

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Documento generato il 20/01/20 alle ore 16:15:26