Document Detail

Effect of vehicle on brain uptake of [11C]toluene.
MedLine Citation:
PMID:  12088732     Owner:  NLM     Status:  MEDLINE    
With the goal of investigating the pharmacokinetics of the abused solvent, toluene we have adapted the rapid coupling of methyl iodide with tributylphenylstannane mediated by palladium(0) complex to the synthesis of no-carrier-added [11C]toluene starting with 11CH(3)I. Two methods for purification and formulation of the tracer were developed. The first one yielded [11C]toluene dissolved in dimethylacetamide/saline solution, for the second one we adapted supercritical fluid technology where the tracer was purified using and conventional C(18) HPLC column and pure supercritical CO(2) fluid as a mobile phase operating at 2000 psi. Formulation of the tracer in cyclodextrin resulted in a significantly higher integrated uptake and distribution volume values. Additionally, we observed higher uptake and slower clearance of 11C-toluene in white matter, consistent with higher lipid content and neurotoxicological evidence indicating restricted and diffuse white matter changes in toluene abusers. This trend was observed when either DMA or cyclodextrin was used as a vehicle. It appears then, that the choice of a vehicle affected only the degree of bioavailability, but not the regional brain pharmacokinetics. Finally, we demonstrated the effect of a decreased percent difference between DV values for the studies performed on the same day, that is, test/retest variability was lower for all brain regions in beta-cyclodextrin experiments. Present results clearly demonstrate that the choice of a vehicle has a significant effect on tracer uptake and should be considered as a potential factor contributing to the pharmacokinetic measurements.
Madina R Gerasimov; Jean Logan; Richard A Ferrieri; Ryan D Muller; David Alexoff; Stephen L Dewey
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  Nuclear medicine and biology     Volume:  29     ISSN:  0969-8051     ISO Abbreviation:  Nucl. Med. Biol.     Publication Date:  2002 Jul 
Date Detail:
Created Date:  2002-06-28     Completed Date:  2003-02-10     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9304420     Medline TA:  Nucl Med Biol     Country:  England    
Other Details:
Languages:  eng     Pagination:  607-12     Citation Subset:  IM    
Brookhaven National Laboratory, Department of Chemistry, Upton, NY 11973, USA.
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MeSH Terms
Acetamides / pharmacology
Brain / metabolism*,  radionuclide imaging
Carbon Radioisotopes / diagnostic use,  isolation & purification,  pharmacokinetics*
Cyclodextrins / pharmacology*
Isotope Labeling / methods*
Radiopharmaceuticals / chemical synthesis,  diagnostic use,  pharmacokinetics
Tissue Distribution
Toluene / diagnostic use,  pharmacokinetics*
Vehicles / pharmacology
Reg. No./Substance:
0/Acetamides; 0/Carbon Radioisotopes; 0/Cyclodextrins; 0/Radiopharmaceuticals; 0/Vehicles; 108-88-3/Toluene; 127-19-5/dimethylacetamide

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