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@INPROCEEDINGS{Elmenhorst:150620,
author = {Elmenhorst, David and Matusch, Andreas and Kroll, Tina and
Bauer, Andreas},
title = {{A}cute ethanol application increases {A}1 adenosine
receptor availability in the human brain},
reportid = {FZJ-2014-00668},
year = {2013},
abstract = {The fatiguing and sedating effects of alcohol in humans are
supposed to be mediated partially by the inhibitory actions
of cerebral adenosine, the main degradation product of ATP.
Ethanol is known to increase extracellular adenosine several
fold in the brain of rats by an increase in adenosine
formation and a decrease of adenosine uptake. Interestingly,
it has recently been reported that cerebral A1 adenosine
receptor (A1AR) availability measured with [11C]MPDX was
increased after ethanol exposure in rats. In the present
pilot study we investigated the impact of acute ethanol
exposure on A1AR availability in the human brain by the use
of PET and the highly selective radioligand [18F]CPFPX. This
method has been proved suitable for quantifying A1AR
densities in the human brain. A bolus plus constant infusion
for steady state quantification allows investigating acute
drug interactions like the occupancy of A1AR by caffeine. In
this ongoing study we administered 40 g of ethanol
(corresponding to 1 L of beer, n=3) or placebo (n=1) during
the steady state period of the PET experiment in healthy
volunteers. Ethanol was diluted in 1 L of isotonic NaCl
solution and infused intravenously between 80 and 110 min of
the 140 min PET scan. Blood alcohol concentration peaked
individually between 0.65 and 0.98 mg/mL 30 min after start
of the infusion. Arterialized venous blood samples were
collected to determine the distribution volume (VT) of
[18F]CPFPX by calculating the ratio of the concentrations
between tissue and plasma during steady state. The timespan
of this ratio represented either baseline (60 to 80 min) or
ethanol condition (120 and 140 min). The distribution
volumes of various cortical and subcortical regions remained
basically constant before and after placebo exposure
(relative difference $3\%).$ In contrast, distribution
volumes in the ethanol group increased quickly by on average
$29\%.$ Our preliminary data exhibit for the first time a
rapid increase in cerebral A1AR availability following acute
intravenous ethanol application in humans.},
month = {May},
date = {2013-05-20},
organization = {The XXVIth International Symposium on
Cerebral Blood Flow, Metabolism and
Function $\&$ XIth International
Conference on Quantification of Brain
Function with PET Xith International
Conference on Quantification of Brain
Function with PET, Shanghai (China), 20
May 2013 - 23 May 2013},
cin = {INM-2},
cid = {I:(DE-Juel1)INM-2-20090406},
pnm = {333 - Pathophysiological Mechanisms of Neurological and
Psychiatric Diseases (POF2-333)},
pid = {G:(DE-HGF)POF2-333},
typ = {PUB:(DE-HGF)1},
url = {https://juser.fz-juelich.de/record/150620},
}