Linked Life Data

10473190

Source:http://linkedlifedata.com/resource/pubmed/id/10473190

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
1999-11-22
pubmed:abstractText
We have identified the value of 18F-fallypride [(S)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-[18F]fluoropropyl)-2, 3-dimethoxybenzamide], as a dopamine D-2 receptor radiotracer for the study of striatal and extrastriatal receptors. Fallypride exhibits high affinities for D-2 and D-3 subtypes and low affinity for D-4 (3H-spiperone IC50s: D-2 = 0.05 nM [rat striata], D-3 = 0.30 nM [SF9 cell lines, rat recombinant], and D-4 = 240 nM [CHO cell lines, human recombinant]). Biodistribution in the rat brain showed localization of 18F-fallypride in striata and extrastriatal regions such as the frontal cortex, parietal cortex, amygdala, hippocampus, thalamus, and hypothalamus. In vitro autoradiographic studies in sagittal slices of the rat brain showed localization of 18F-fallypride in striatal and several extrastriatal regions, including the medulla. Positron emission tomography (PET) experiments with 18F-fallypride in male rhesus monkeys were carried out in a PET VI scanner. In several PET experiments, apart from the specific binding seen in the striatum, specific binding of 18F-fallypride was also identified in extracellular regions (in a lower brain slice, possibly the thalamus). Specific binding in the extrastriata was, however, significantly lower compared with that observed in the striata of the monkeys (extrastriata/cerebellum = 2, striata/cerebellum = 10). Postmortem analysis of the monkey brain revealed significant 18F-fallypride binding in the striata, whereas binding was also observed in extrastriatal regions such as the thalamus, cortical areas, and brain stem.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0969-8051
pubmed:author
pubmed:issnType
Print
pubmed:volume
26
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
519-27
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:10473190-Animals, pubmed-meshheading:10473190-Autoradiography, pubmed-meshheading:10473190-Benzamides, pubmed-meshheading:10473190-Brain, pubmed-meshheading:10473190-Cell Line, pubmed-meshheading:10473190-Corpus Striatum, pubmed-meshheading:10473190-Fluorine Radioisotopes, pubmed-meshheading:10473190-Humans, pubmed-meshheading:10473190-Macaca mulatta, pubmed-meshheading:10473190-Male, pubmed-meshheading:10473190-Pyrrolidines, pubmed-meshheading:10473190-Radioligand Assay, pubmed-meshheading:10473190-Rats, pubmed-meshheading:10473190-Rats, Sprague-Dawley, pubmed-meshheading:10473190-Receptors, Dopamine D2, pubmed-meshheading:10473190-Receptors, Dopamine D3, pubmed-meshheading:10473190-Recombinant Proteins, pubmed-meshheading:10473190-Tissue Distribution, pubmed-meshheading:10473190-Tomography, Emission-Computed, pubmed-meshheading:10473190-Transfection
pubmed:year
1999
pubmed:articleTitle
Preliminary assessment of extrastriatal dopamine D-2 receptor binding in the rodent and nonhuman primate brains using the high affinity radioligand, 18F-fallypride.
pubmed:affiliation
Department of Radiology, Franklin McLean Institute, University of Chicago, Illinois, USA. jogeshwar-mukherjee@ketthealth.com
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, Non-P.H.S.