%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