Linked Life Data

10363802

Source:http://linkedlifedata.com/resource/pubmed/id/10363802

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1999-7-29
pubmed:abstractText
Previous research into development of a gallium-radiolabeled agent that crosses the blood-brain barrier has met with limited success. In this study, we focused our attention on a Ga(III) complex of a 4-coordinate amine trithiolate tripod ligand, tris(2-mercaptobenzyl) amine (S3N). The Ga(III) S3N complex is small, neutral, and lipophilic, meeting the requirements for a potential brain imaging agent. The Ga-68 complex was easily formed with a radiochemical purity of >95%. In vitro stability of the Ga-S3N complex, determined in rat serum incubated at 37 degrees C, was greater than 95% intact at 2 h by silica gel and reversed-phase radio-thin layer chromatography. Biodistribution studies conducted in female Sprague-Dawley rats showed the complex cleared rapidly from the blood with initial high liver uptake followed by rapid washout. Significant uptake was observed in the brain, with brain:blood ratios increasing from 0.11 at 2 min postinjection to 3.8 at 60 min postinjection. Uptake was also observed in the heart going from a heart:blood ratio of 2.3 at 2 min postinjection to 11 at 60 min postinjection. Molecular mechanics were used to determine the coordination number, and demonstrated that the Ga(III) complex prefers to be 4-coordinate. Imaging studies with 68Ga-S3N in a Nemestrina macaque showed significant brain uptake, similar to other lipophilic agents. The extraction of 68Ga-S3N into the brains of both rodents and primates, higher than any 68Ga agent reported in the literature, suggests that this compound may have potential as a brain imaging agent for positron emission tomography.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0969-8051
pubmed:author
pubmed:issnType
Print
pubmed:volume
26
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
305-16
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:10363802-Animals, pubmed-meshheading:10363802-Autoradiography, pubmed-meshheading:10363802-Blood-Brain Barrier, pubmed-meshheading:10363802-Brain, pubmed-meshheading:10363802-Carbon Radioisotopes, pubmed-meshheading:10363802-Cricetinae, pubmed-meshheading:10363802-Dogs, pubmed-meshheading:10363802-Drug Stability, pubmed-meshheading:10363802-Ethanol, pubmed-meshheading:10363802-Female, pubmed-meshheading:10363802-Gallium Radioisotopes, pubmed-meshheading:10363802-Heart, pubmed-meshheading:10363802-Lung, pubmed-meshheading:10363802-Macaca nemestrina, pubmed-meshheading:10363802-Male, pubmed-meshheading:10363802-Mesocricetus, pubmed-meshheading:10363802-Myocardium, pubmed-meshheading:10363802-Organometallic Compounds, pubmed-meshheading:10363802-Radiopharmaceuticals, pubmed-meshheading:10363802-Rats, pubmed-meshheading:10363802-Rats, Sprague-Dawley, pubmed-meshheading:10363802-Thiosemicarbazones, pubmed-meshheading:10363802-Tissue Distribution, pubmed-meshheading:10363802-Tomography, Emission-Computed
pubmed:year
1999
pubmed:articleTitle
Evaluation of gallium-68 tris(2-mercaptobenzyl)amine: a complex with brain and myocardial uptake.
pubmed:affiliation
The Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri 63110, USA.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, Non-P.H.S.