PET neuroimaging with [11C]venlafaxine: serotonin uptake inhibition, biodistribution and binding in living pig brain.
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PET neuroimaging with [11C]venlafaxine: serotonin uptake inhibition, biodistribution and binding in living pig brain. / Smith, D F; Jensen, P N; Gee, A D; Hansen, Søren Baarsgaard; Danielsen, E; Andersen, Flemming; Saiz, P A; Gjedde, A.
In: European Neuropsychopharmacology, Vol. 7, No. 3, 1997, p. 195-200.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - PET neuroimaging with [11C]venlafaxine: serotonin uptake inhibition, biodistribution and binding in living pig brain.
AU - Smith, D F
AU - Jensen, P N
AU - Gee, A D
AU - Hansen, Søren Baarsgaard
AU - Danielsen, E
AU - Andersen, Flemming
AU - Saiz, P A
AU - Gjedde, A
PY - 1997
Y1 - 1997
N2 - The brain binding kinetics and distribution of the antidepressant venlafaxine, labelled with 11C in the O-methyl position, was studied by PET after intravenous injection in anesthetized pigs. In addition, venlafaxine's action on serotonin (5-HT) uptake was studied in vitro in blood platelets obtain from humans or pigs. Venlafaxine resembled imipramine, paroxetine and citalopram in causing a dose-dependent inhibition of 5-HT uptake in blood platelets from pigs and humans. Venlafaxine-derived radioactivity entered the living brain readily and showed higher binding potentials in diencephalic and telencephalic regions than in cerebellum. Acute administration of an antidepressant drug (i.e. imipramine, citalopram or paroxetine) enhanced the distribution and altered the binding of venlafaxine in certain brain regions. The findings show that [11C]venlafaxine is not an ideal PET radiotracer mainly because of its relatively low binding potentials and its lack of specificity for the 5-HT transporter in living brain.
AB - The brain binding kinetics and distribution of the antidepressant venlafaxine, labelled with 11C in the O-methyl position, was studied by PET after intravenous injection in anesthetized pigs. In addition, venlafaxine's action on serotonin (5-HT) uptake was studied in vitro in blood platelets obtain from humans or pigs. Venlafaxine resembled imipramine, paroxetine and citalopram in causing a dose-dependent inhibition of 5-HT uptake in blood platelets from pigs and humans. Venlafaxine-derived radioactivity entered the living brain readily and showed higher binding potentials in diencephalic and telencephalic regions than in cerebellum. Acute administration of an antidepressant drug (i.e. imipramine, citalopram or paroxetine) enhanced the distribution and altered the binding of venlafaxine in certain brain regions. The findings show that [11C]venlafaxine is not an ideal PET radiotracer mainly because of its relatively low binding potentials and its lack of specificity for the 5-HT transporter in living brain.
M3 - Journal article
C2 - 9213078
VL - 7
SP - 195
EP - 200
JO - European Neuropsychopharmacology
JF - European Neuropsychopharmacology
SN - 0924-977X
IS - 3
ER -
ID: 14946229