1252762-31-4Relevant articles and documents
Synthesis and Evaluation of a New 18F-Labeled Radiotracer for Studying the GABAB Receptor in the Mouse Brain
Naik, Ravi,Valentine, Heather,Dannals, Robert F.,Wong, Dean F.,Horti, Andrew G.
, p. 1453 - 1461 (2018/06/26)
New GABAB agonists, fluoropyridyl ether analogues of baclofen, have been synthesized as potential PET radiotracers. The compound with highest inhibition binding affinity as well as greatest agonist response, (R)-4-amino-3-(4-chloro-3-((2-fluoro
Discovery of a novel potent GABAB receptor agonist
Xu, Feng,Peng, Ge,Phan, Thu,Dilip, Usha,Chen, Jian Lu,Chernov-Rogan, Tania,Zhang, Xuexiang,Grindstaff, Kent,Annamalai, Thamil,Koller, Kerry,Gallop, Mark A.,Wustrow, David J.
scheme or table, p. 6582 - 6585 (2011/12/04)
Structure-activity studies have led to a discovery of 3-(4-pyridyl)methyl ether derivative 9d that has 25-to 50-fold greater functional potency than R-baclofen at human and rodent GABAB receptors in vitro. Mouse hypothermia studies confirm that this compound crosses the blood-brain barrier and is approximately 50-fold more potent after systemic administration.
GAMMA-AMINO-BUTYRIC ACID DERIVATIVES AS GABAB RECEPTOR LIGANDS
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Page/Page column 52, (2010/11/03)
Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.