TY  - JOUR
AU  - Boy, Christian
AU  - Klimke, Ansgar
AU  - Holschbach, Markus
AU  - Herzog, Hans
AU  - Mühlensiepen, Heinz
AU  - Rota Kops, Elena
AU  - Sonnenberg, Frank
AU  - Gaebel, Wolfgang
AU  - Stöcklin, Gerhard
AU  - Markstein, Rudolf
AU  - Müller-Gärtner, Hans-W.
TI  - Imaging Dopamine D4 Receptors in the Living Primate Brain: A Positron Emission Tomography Study Using the Novel D1/D4 Antagonist [11C]SDZ GLC 756
JO  - Synapse
VL  - 30
PB  - Wiley
M1  - PreJuSER-136190
SP  - 341–350
N1  - Record converted from JUWEL: 18.07.2013
AB  - The dopamine D4 receptor has lately attracted interest since it has been
AB  - hypothesized to be involved in the pathogenesis and pharmacotherapy of neuropsychiatric diseases. The present study provides first in vivo evidence of dopamine D4 receptors in primate brain using a [11C]benzo[g]quinoline, the novel radioligand [11C]SDZ GLC 756 ([11C]GLC: in vitro dissociation constants at human receptor clones [nM]: 1.10 at D1; 0.40
AB  - at D2; 25 at D3; 0.18 at D4.2; 6.03 at D5). Dynamic positron emission tomography scans
AB  - were performed on healthy baboons (Papio hamadryas, n 5 3). Specific receptor binding
AB  - (SB) was calculated for striatum and neocortex (frontal, temporal, parietal, and occipital) based on the differences between the regional and the cerebellar concentration of [11C].
AB  - Blockade of D1 and D5 receptors by SCH23390 (1.7 μmol/kg) diminished SB in the
AB  - striatum by 55 6 4% (mean 6 standard deviation, P , 0.05) and in the frontal cortex by 13 6 8% (P , 0.05) when compared to SB in the unblocked state (SBD1–D5). In the presence of the dopamine antagonists SCH23390 (1.7 μmol/kg) and raclopride (5.7
AB  - μmol/kg)—which mask the D1, D2, D3, and D5 subtypes—SB of [11C]GLC to D4 receptors
AB  - (SBD4) was demonstrated in the striatum and all cortical regions of interest. In the
AB  - striatum, the ratio of SBD4/SBD1–D5 was 0.13 6 0.07. In the neocortex, SBD4/SBD1–D5 was
AB  - notably higher (0.77 60.29; mean of all cortical regions of interest). The widespread
AB  - distribution of dopamine D4 receptors suggests a basic functional role of this receptor subtype in the modulation of cortical and subcortical neuronal activity
LB  - PUB:(DE-HGF)16
UR  - https://juser.fz-juelich.de/record/136190
ER  -