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ACS chemical neuroscience v.8 no.1, 2017년, pp.22 - 27   SCIE
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Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites

Jensen, Claus H. (Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, ) ; Hansen, Hanne D. (Neurobiology Research Unit and Center for Integrated Molecular Brain Imaging, Rigshospitalet and University of Copenhagen, Blegdamsvej 9, 2100 Copenhagen, ) ; Bay, Tina (Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, ) ; Vogensen, Stine B. (Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, ) ; Lehel, Szabolcs (PET and Cyclotron Unit, Copenhagen University Hospital, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, ) ; Thiesen, Louise (Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, ) ; Bundgaard, Christoffer (Discovery DMPK, H. Lundbeck A/S, Ottiliavej, 2500 Valby, ) ; Clausen, Rasmus P. (Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, ) ; Knudsen, Gitte M. (Neurobiology Research Unit and Ce ) ; Herth, Matthias M. ; Wellendorph, Petrine ; Frølund, Bente ;
  • 초록  

    γ-Hydroxybutyric acid (GHB) is an endogenous neuroactive substance and proposed neurotransmitter with affinity for both low- and high-affinity binding sites. A radioligand with high and specific affinity toward the high-affinity GHB binding site would be a unique tool toward a more complete understanding of this population of binding sites. With its high specific affinity and monocarboxylate transporter (MCT1) mediated transport across the blood-brain barrier in pharmacological doses, 3-hydroxycyclopent-1-enecarboxylic acid (HOCPCA) seems like a suitable PET radiotracer candidate. Here, we report the 11 C-labeling and subsequent evaluation of [ 11 C]HOCPCA in a domestic pig, as a PET-radioligand for visualization of the high-affinity GHB binding sites in the live pig brain. To investigate the regional binding of HOCPCA in pig brain prior to in vivo PET studies, in vitro quantitative autoradiography on sections of pig brain was performed using [ 3 H]HOCPCA. In vivo evaluation of [ 11 C]HOCPCA showed no brain uptake, possibly due to a limited uptake of HOCPCA by the MCT1 transporter at tracer doses of [ 11 C]HOCPCA. Graphic Abstract ACS Electronic Supporting Info


  • 주제어

    GHB .   HOCPCA .   GHB binding site distribution .   PET .   in vitro autoradiography.  

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