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Titolo:
IMAGING DOPAMINE D-4 RECEPTORS IN THE LIVING PRIMATE BRAIN - A POSITRON-EMISSION-TOMOGRAPHY STUDY USING THE NOVEL D-1 D-4 ANTAGONIST [C-11]SDZ-GLC-756/
Autore:
BOY C; KLIMKE A; HOLSCHBACH M; HERZOG H; MUHLENSIEPEN H; KOPS ER; SONNENBERG F; GAEBEL W; STOCKLIN G; MARKSTEIN R; MULLERGARTNER HW;
Indirizzi:
KFA JULICH GMBH,RES CTR,INST MED D-52425 JULICH GERMANY UNIV DUSSELDORF,CLIN NUCL MED D-40225 DUSSELDORF GERMANY UNIV DUSSELDORF,DEPT PSYCHIAT D-40225 DUSSELDORF GERMANY KFA JULICH GMBH,RES CTR,INST NUCL CHEM D-52425 JULICH GERMANY NOVARTIS PHARMA AG,NERVOUS SYST RES CH-4002 BASEL SWITZERLAND
Titolo Testata:
Synapse
fascicolo: 4, volume: 30, anno: 1998,
pagine: 341 - 350
SICI:
0887-4476(1998)30:4<341:IDDRIT>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
MOLECULAR-BIOLOGY; CEREBRAL-CORTEX; D4 RECEPTORS; SCHIZOPHRENIA; SITES; BINDING; RACLOPRIDE; PET;
Keywords:
POSITRON EMISSION TOMOGRAPHY; DOPAMINE RECEPTORS; DOPAMINE D-4 RECEPTORS; SCH23390; RACLOPRIDE; SPIPERONE; BABOON; NONHUMAN PRIMATES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
C. Boy et al., "IMAGING DOPAMINE D-4 RECEPTORS IN THE LIVING PRIMATE BRAIN - A POSITRON-EMISSION-TOMOGRAPHY STUDY USING THE NOVEL D-1 D-4 ANTAGONIST [C-11]SDZ-GLC-756/", Synapse, 30(4), 1998, pp. 341-350

Abstract

The dopamine D-4 receptor has lately attracted interest since it has been hypothesized to be involved in the pathogenesis and pharmacotherapy of neurapsychiatric diseases. The present study provides first in vivo evidence of dopamine D-4 receptors in primate brain using a [C-11]benzo[g]quinoline, the novel radioligand [C-11]SDZ GLC 756 ([C-11] GLC: in vitro dissociation constants at human receptor clones [nM]: 1.10 at D-1; 0.40 at D-2; 25 at D-3; 0.18 at D-4.2; 6.03 at D-5) Dynamic positron emission tomography scans were performed on healthy baboons (Papio hamadryas, n = 3). Specific receptor binding (SB) was calculated for striatum and neocortex (frontal, temporal, parietal, and occipital)based on the differences between the regional and the cerebellar concentration of [C-11]. Blockade of D-1 and D-6 receptors by SCH23390 (1.7 mu mol/kg) diminished SE in the striatum by 55 +/- 4% (mean +/- standard deviation, P < 0.05) and in the frontal cortex by 13 +/- 8% (P < 0.05) when compared to SE in the unblocked state (SBD1-D5) In the presence of the dopamine antagonists SCH23390 (1.7 mu mol/kg) and raclopride (5.7 mu mol/kg)-which mask the D-1, D-2, D-3, and D-5 subtypes-SB of [C-11]GLC to D-4 receptors (SBD4) was demonstrated in the striatum and all cortical regions of interest. In the striatum, the ratio of SBD4/SBD1-D5 was 0.13 +/- 0.07. In the neocortex, SBD4/SBD1-D5 was notably higher (0.77 +/- 0.29; mean of all cortical regions of interest). The widespread distribution of dopamine D-4 receptors suggests a basic functional role of this receptor subtype in the modulation of cortical and subcortical neuronal activity. (C) 1998 Wiley-Liss, Inc.

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Documento generato il 17/01/20 alle ore 21:15:37