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Background. Marijuana acts by stimulating the cannabinoid CB1 receptor in brain. This receptor has recently been the target for theraputuc drug development – e.g., drugs that can reduce appetite or suppress the urge to smoke cigarettes. Although the CB1 receptor is one of the most abundant in the central nervous system, developing an effective PET ligand has been very difficult. In collaboration with the pharmaceutical company Eli Lilly, we developed a promising PET radioligand that has binds reversibly and with high specific signal in monkey brain (Yasuno et al., 2008). Preliminary results in healthy subjects are promising for this radioligand [11C]MePPEP.
Legend. PET summation image in rhesus brain following injection of [11C]MePPEP. PET images (middle column) were summed from 60 to 120 min. The corresponding MR images are on left column, and the fused PET and MR images are on right column. Upper row: slice including cerebellum and medial and lateral temporal cortex. Middle row: slice including striatum, thalamus, and lateral temporal cortex. Lower row: slice including prefrontal cortex.
Reference. F. Yasuno, A.K. Brown, S.S. Zoghbi, J.H. Krushinski, E. Chernet, J. Tauscher, J.M. Schaus, L.A. Phebus, A.K. Chesterfield, C.C. Felder, R.L. Gladding, J. Hong, C. Halldin, V.W. Pike, and R.B. Innis. The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain. Neuropsychopharmacology,
33: 259-269, 2008. Download PDF Reference (316 kb.)
Garth Terry, Jeih-San Liow, Eyassu Chernet, Sami S. Zoghbi, Lee Phebus, Christian C. Felder, Johannes Tauscher, John M. Schaus, Victor W. Pike, Christer Halldin, and Robert B. Innis. Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodents. NeuroImage 41, 690–698, 2008. Download PDF Reference (498 kb.)
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