Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1989-3-17
pubmed:abstractText
The S and R enantiomers of the psychotomimetic 5HT2 agonist DOI (2,5-dimethoxy-4-iodophenylisopropylamine) were labeled with 125I at high-specific activity. The regional distribution of binding sites for each of the enantiomers was investigated using in vitro quantitative autoradiography and compared to the regional distribution of [125I]LSD in the rat brain. Saturable, specific binding of the radioligands was determined in cortical membrane homogenates. All radioligands exhibited specific binding in localized regions throughout the rat brain. Binding of [125I]DOI enantiomers was completely displaced (greater than 90%) by 1 microM of the corresponding unlabeled enantiomer; [125I]LSD was completely displaced by 1 microM LSD. The choroid plexus showed the highest-density binding. Other regions showing high-density binding included the frontoparietal cortex (motor and somatosensory areas), anterior cingulate gyrus, lateral olfactory tubercle, nucleus accumbens, caudate nuclei, claustrum, nucleus of the lateral olfactory tract, dentate gyrus, mamillary nuclei, and motor trigeminal nuclei. In most regions, [125I]S-DOI, the less active enantiomer, exhibited 25-40% of the amount of total binding as [125I]R-DOI. In some regions, [125I]R-DOI and [125I]LSD had similar binding densities; in others, marked differences were apparent. The regional distribution of specific [125I]R-DOI binding sites correlated with the distribution of 5HT2 receptors reported in previous studies. DOI and its analogs may have potential clinical applications for in vivo localization of 5HT2-receptors using positron emission tomography (PET) and similar techniques.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0006-8993
pubmed:author
pubmed:issnType
Print
pubmed:day
2
pubmed:volume
476
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
45-56
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Common receptors for hallucinogens in rat brain: a comparative autoradiographic study using [125I]LSD and [125I]DOI, a new psychotomimetic radioligand.
pubmed:affiliation
Laboratory of Clinical Science, National Institute of Mental Health, Bethesda, MD 20892.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't