[11C]AZ10419369: A selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in the primate brain

NeuroImage ◽  
2008 ◽  
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Jan Andersson ◽  
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Dennis J. McCarthy ◽  
Sjoerd J. Finnema ◽  
...  
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Carl-Gunnar Swahn ◽  
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Martine Guillermier ◽  
Stéphane Demphel ◽  
...  

1995 ◽  
Vol 15 (5) ◽  
pp. 798-805 ◽  
Author(s):  
Zsolt Szabo ◽  
Ursula Scheffel ◽  
Makiko Suehiro ◽  
Robert F. Dannals ◽  
Sang Eun Kim ◽  
...  

[C]McN5652 is a new radioligand specific for 5-hydroxytryptamine (5-HT; serotonin) transporters. In this study we used [11C]McN5652 to image the 5-HT transporter sites in baboon brain by positron emission tomography (PET). Dynamic PET studies were performed in three Papio anubis baboons. The animals were injected intravenously first with 11C-labeled (+)-McN5652([11C](+)McN5652), then with pharmacologically inactive enantiomer 11C-labeled (–)-McN5652 ([11C](–)McN5652); two animals received a third study with [11C](+)McN5652 after pretreatment with the specific 5-HT uptake site inhibitor fluoxetine (5 mg/kg). Initial uptake into the brain was similar for both [11C](+)McN5652 and [11C](–)McN5652. At later times (45–120 min after injection), only [11C](+)McN5652 showed a distribution characteristic for 5-HT uptake sites. In contrast, in studies with [11C](–)McN5652 and in those with [11C](+)McN5652 after 5-HT uptake site blockade with fluoxetine, 11C radioactivity concentrations were significantly lower and the distribution pattern was relatively even. The differences between [11C](+)-and (–)McN5652 were calculated for the time interval 95–125 min postinjection and used to estimate specific binding. Specific binding correlated well ( r = 0.95, p < 0.001) with the known density of 5-HT uptake sites in human brain. These results indicate that [11C](+)McN5652 is suitable for PET imaging of 5-HT uptake sites in primate brain.


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