Imaging and Quantitation of Cannabinoid CB1 Receptors in Human and Monkey Brains Using 18F-Labeled Inverse Agonist Radioligands

We recently demonstrated that 11 C-MePPEP, a PET ligand for CB 1 receptors, has such high uptake in the human brain that it can be imaged for 210 min and that receptor density can be quantified as distribution volume ( V T ) using the gold standard of compartmental modeling. However, 11 C-MePPEP had...

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Published inThe Journal of nuclear medicine (1978) Vol. 51; no. 1; pp. 112 - 120
Main Authors Terry, Garth E, Hirvonen, Jussi, Liow, Jeih-San, Zoghbi, Sami S, Gladding, Robert, Tauscher, Johannes T, Schaus, John M, Phebus, Lee, Felder, Christian C, Morse, Cheryl L, Donohue, Sean R, Pike, Victor W, Halldin, Christer, Innis, Robert B
Format Journal Article
LanguageEnglish
Published Soc Nuclear Med 01.01.2010
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Summary:We recently demonstrated that 11 C-MePPEP, a PET ligand for CB 1 receptors, has such high uptake in the human brain that it can be imaged for 210 min and that receptor density can be quantified as distribution volume ( V T ) using the gold standard of compartmental modeling. However, 11 C-MePPEP had relatively poor retest and intersubject variabilities, which were likely caused by errors in the measurements of radioligand in plasma at low concentrations by 120 min. We sought to find an analog of 11 C-MePPEP that would provide more accurate plasma measurements. We evaluated several promising analogs in the monkey brain and chose the 18 F-di-deutero fluoromethoxy analog ( 18 F-FMPEP- d 2 ) to evaluate further in the human brain.
ISSN:0161-5505
1535-5667
DOI:10.2967/jnumed.109.067074