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@ARTICLE{Boy:136190,
author = {Boy, Christian and Klimke, Ansgar and Holschbach, Markus
and Herzog, Hans and Mühlensiepen, Heinz and Rota Kops,
Elena and Sonnenberg, Frank and Gaebel, Wolfgang and
Stöcklin, Gerhard and Markstein, Rudolf and
Müller-Gärtner, Hans-W.},
title = {{I}maging {D}opamine {D}4 {R}eceptors in the {L}iving
{P}rimate {B}rain: {A} {P}ositron {E}mission {T}omography
{S}tudy {U}sing the {N}ovel {D}1/{D}4 {A}ntagonist
[11{C}]{SDZ} {GLC} 756},
journal = {Synapse},
volume = {30},
publisher = {Wiley},
reportid = {PreJuSER-136190},
pages = {341–350},
note = {Record converted from JUWEL: 18.07.2013},
comment = {Synapse 30:341–350},
booktitle = {Synapse 30:341–350},
abstract = {The dopamine D4 receptor has lately attracted interest
since it has been 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 at D2; 25 at D3; 0.18
at D4.2; 6.03 at D5). Dynamic positron emission tomography
scans were performed on healthy baboons (Papio hamadryas, n
5 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 [11C]. Blockade of D1 and D5
receptors by SCH23390 (1.7 μmol/kg) diminished SB in the
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 μmol/kg)—which mask the D1, D2, D3,
and D5 subtypes—SB of [11C]GLC to D4 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 6 0.07. In the neocortex, SBD4/SBD1–D5 was notably
higher (0.77 60.29; mean of all cortical regions of
interest). The widespread distribution of dopamine D4
receptors suggests a basic functional role of this receptor
subtype in the modulation of cortical and subcortical
neuronal activity},
cin = {INM-4},
ddc = {500},
cid = {I:(DE-Juel1)INM-4-20090406},
typ = {PUB:(DE-HGF)16},
url = {https://juser.fz-juelich.de/record/136190},
}