ISSN:
1435-1463
Keywords:
[3H]Nemonapride
;
dopamine D2 receptors
;
PET
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary We characterized [3H]nemonapride ([3H]NEM, [3H]YM-09151-2) binding to dopamine D2 receptors. In mice given [3H]NEM with and without sulpiride, thein vivo specific binding of the [3H]NEM to the D2 receptors in the striatum was assessed: SBin vivo-1, striatal uptake minus cerebellar uptake; and SBin vivo-2, uptake in the control mice minus uptake in the sulpiride-treated mice. Tissue homogenates were divided into cytosol and the membrane binding fraction (MB). When the MB was incubatedin vitro with sulpiride, the dissociated and nondissociated fractions were defined as theex vivospecific binding (SBex vivo) and theex vivo nonspecific binding (NBex vovo), respectively. HPLC revealed that most of the radioactivity in the MB was [3H]NEM, whereas metabolites were found in the cytosol. In the striatum, the SBex vivo increased with time (50% of the total tissue uptake at 60 min), and was equivalent to the SBin vivo-2. The SBin vivo-1 was comparable to the MB. In the cerebral cortex and cerebellum, the SBex vivo decreased with time and the SBex vivo/free [3H]NEM ratios were smaller than those in the striatum.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01277948
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