Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites
| Autor: | Gitte M. Knudsen, Matthias M. Herth, Claus H. Jensen, Tina Bay, Rasmus P. Clausen, Szabolcs Lehel, Christoffer Bundgaard, Stine B. Vogensen, Bente Frølund, Petrine Wellendorph, Hanne D. Hansen, Louise Thiesen |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Monocarboxylate transporter
education.field_of_study biology 010405 organic chemistry Physiology Chemistry Cognitive Neuroscience Radiosynthesis Population Cell Biology General Medicine 01 natural sciences Biochemistry In vitro 0104 chemical sciences 03 medical and health sciences 0302 clinical medicine In vivo Mediated transport Radioligand biology.protein Binding site education 030217 neurology & neurosurgery |
| Zdroj: | ACS Chemical Neuroscience. 8:22-27 |
| ISSN: | 1948-7193 |
| Popis: | 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 11C-labeling and subsequent evaluation of [11C]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 [3H]HOCPCA. In vivo evaluation of [11C]HOCPCA showed no brain upta... |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|