ncs-382 has been researched along with 3-hydroxycyclopent-1-enecarboxylic-acid* in 1 studies
1 other study(ies) available for ncs-382 and 3-hydroxycyclopent-1-enecarboxylic-acid
| Article | Year |
|---|---|
New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.
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 [(3)H]-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 [(3)H]-1 binding shows high specificity to the high-affinity GHB binding sites. Topics: Animals; Benzocycloheptenes; Binding Sites; Binding, Competitive; Brain; Carboxylic Acids; Cell Line; Central Nervous System; Cyclopentanes; Drug Stability; gamma-Aminobutyric Acid; Hydroxybutyrates; Kinetics; Ligands; Male; Models, Chemical; Molecular Structure; Radioligand Assay; Rats; Rats, Sprague-Dawley; Synaptic Membranes; Tritium | 2013 |