Journal of medicinal chemistry, 2013-10, Vol.56 (20), p.8201-8205
2013
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity γ‑Hydroxybutyrate (GHB) Binding Sites
- Ist Teil von
- Journal of medicinal chemistry, 2013-10, Vol.56 (20), p.8201-8205
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2013
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm4011719Titel-ID: cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_3888956
- Format
- –
- Schlagworte
- Animals, Benzocycloheptenes - chemistry, Benzocycloheptenes - metabolism, Binding Sites, Binding, Competitive, Brain - metabolism, Carboxylic Acids - chemical synthesis, Carboxylic Acids - chemistry, Carboxylic Acids - metabolism, Cell Line, Central Nervous System - metabolism, Cyclopentanes - chemical synthesis, Cyclopentanes - chemistry, Cyclopentanes - metabolism, Drug Stability, gamma-Aminobutyric Acid - chemistry, gamma-Aminobutyric Acid - metabolism, Hydroxybutyrates - chemistry, Hydroxybutyrates - metabolism, Kinetics, Ligands, Male, Models, Chemical, Molecular Structure, Radioligand Assay, Rats, Rats, Sprague-Dawley, Synaptic Membranes - metabolism, Tritium - metabolism