An acute effect of triazolam on muscarinic cholinergic receptor binding in the human brain measured by positron emission tomography

1994 ◽  
Vol 113 (3-4) ◽  
pp. 311-317 ◽  
Author(s):  
Tetsuya Suhara ◽  
Osamu Inoue ◽  
Kaoru Kobayashi ◽  
Toshiyuki Satoh ◽  
Yukio Tateno
1999 ◽  
Vol 19 (9) ◽  
pp. 956-966 ◽  
Author(s):  
Justin S. Smith ◽  
Jon-Kar Zubieta ◽  
Julie C. Price ◽  
John E. Flesher ◽  
Igal Madar ◽  
...  

The regional binding of N1′ -([11C]methyl)naltrindole (MeNTI), a selective δ-opioid antagonist, was studied in healthy human subjects with positron emission tomography (PET). After the bolus intravenous administration of high specific activity [11C]MeNTI, PET was performed over 90 minutes. Arterial plasma samples were obtained during the scanning period and assayed for the presence of radiolabeled metabolites. The data were analyzed with various kinetic (two-and three-compartment models, Patlak graphical analysis) and nonkinetic (apparent volume of distribution and activity at a late scanning time) approaches. This tracer showed irreversible binding characteristics during the scanning period used. The results of the analyses also were compared with the density and distribution of δ-opioid receptors in the human brain in vitro. Additionally, computer simulations were performed to assess the effects of changes in receptor binding and tracer transport changes on the perceived binding parameters obtained with the models. A constrained three-compartment kinetic model was demonstrated to be superior to other quantification models for the description of MeNTI kinetics and quantification of δ receptor binding in the human brain with 11C-labeled MeNTI.


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