%0 Journal Article %A Vogensen, Stine B. %A Marek, Aleš %A Bay, Tina %A Wellendorph, Petrine %A Kehler, Jan %A Bundgaard, Christoffer %A Frølund, Bente %A H. F. Pedersen, Martin %A Clausen, Rasmus P. %D 2013 %T New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity γ‑Hydroxybutyrate (GHB) Binding Sites %U https://acs.figshare.com/articles/journal_contribution/New_Synthesis_and_Tritium_Labeling_of_a_Selective_Ligand_for_Studying_High_Affinity_Hydroxybutyrate_GHB_Binding_Sites/2362846 %R 10.1021/jm4011719.s001 %2 https://acs.figshare.com/ndownloader/files/4002289 %K Selective Ligand %K binding %K site %K GHB %K New Synthesis %K lithium trimethoxyborotritide %K HOCPCA %K vivo brain penetration %K CNS targets %K synthesis %X 3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [3H]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity, and we demonstrate in vivo brain penetration. In vitro characterization of [3H]-1 binding shows high specificity to the high-affinity GHB binding sites. %I ACS Publications