PET neuroimaging with [11C]venlafaxine: serotonin uptake inhibition, biodistribution and binding in living pig brain.

D F Smith; P N Jensen; A D Gee; Søren Baarsgaard Hansen; E Danielsen; Flemming Andersen; P A Saiz; A Gjedde

PET neuroimaging with [11C]venlafaxine: serotonin uptake inhibition, biodistribution and binding in living pig brain.

D F Smith, P N Jensen, A D Gee, Søren Baarsgaard Hansen, E Danielsen, Flemming Andersen, P A Saiz, A Gjedde

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

32 Citationer (Scopus)

Abstract

Udgivelsesdato: 1997-Aug

Originalsprog	Engelsk
Tidsskrift	European Neuropsychopharmacology
Vol/bind	7
Udgave nummer	3
Sider (fra-til)	195-200
Antal sider	5
ISSN	0924-977X
Status	Udgivet - 1997
Udgivet eksternt	Ja

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Citationsformater

@article{37856df0b31511debc73000ea68e967b,

title = "PET neuroimaging with [11C]venlafaxine: serotonin uptake inhibition, biodistribution and binding in living pig brain.",

abstract = "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.",

author = "Smith, {D F} and Jensen, {P N} and Gee, {A D} and Hansen, {S{\o}ren Baarsgaard} and E Danielsen and Flemming Andersen and Saiz, {P A} and A Gjedde",

year = "1997",

language = "English",

volume = "7",

pages = "195--200",

journal = "European Neuropsychopharmacology",

issn = "0924-977X",

publisher = "Elsevier",

number = "3",

}

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

SN - 0924-977X

VL - 7

SP - 195

EP - 200

JO - European Neuropsychopharmacology

JF - European Neuropsychopharmacology

IS - 3

ER -