[18F]haloperidol binding in baboon brain in vivo.
The binding of [18F]haloperidol to dopamine D2 and to sigma recognition sites in baboon brain was examined using positron emission tomography (PET). Studies were performed at baseline and after treatment with either haloperidol (to evaluate saturability), (+)-butaclamol (which has specificity for dopamine D2 receptors) or (-)-butaclamol (which has specificity for sigma sites). Binding was widespread. Treatment with (-)-butaclamol had no effect, whereas (+)-butaclamol selectively reduced the uptake in striatum. Haloperidol increased the clearance rate from all brain regions. These results indicate that the binding profile of [18F]haloperidol does not permit the selective examination of either dopamine D2 or sigma sites using PET.
Yousef
K A
KA
Chemistry Department, Brookhaven National Laboratory, Upton, NY 11973, USA.
Fowler
J S
JS
Volkow
N D
ND
Dewey
S L
SL
Shea
C
C
Schlyer
D J
DJ
Gatley
S J
SJ
Logan
J
J
Wolf
A P
AP
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002069:Butaclamol / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000097:blood / Q000493:pharmacokinetics*; D005462:Fluorine Radioisotopes; D006220:Haloperidol / Q000097:blood / Q000493:pharmacokinetics*; D007553:Isotope Labeling; D010215:Papio; D017448:Receptors, Dopamine D2 / Q000187:drug effects / Q000378:metabolism; D014055:Tomography, Emission-Computed
D018492:Dopamine Antagonists; D005462:Fluorine Radioisotopes; D017448:Receptors, Dopamine D2; D002069:Butaclamol; D006220:Haloperidol