Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2011 Nov 1;21(21):6582-5.
doi: 10.1016/j.bmcl.2011.08.006. Epub 2011 Aug 17.

Discovery of a novel potent GABA(B) receptor agonist

Feng Xu  1 , Ge Peng, Thu Phan, Usha Dilip, Jian Lu Chen, Tania Chernov-Rogan, Xuexiang Zhang, Kent Grindstaff, Thamil Annamalai, Kerry Koller, Mark A Gallop, David J Wustrow
Affiliations

Discovery of a novel potent GABA(B) receptor agonist

Feng Xu et al. Bioorg Med Chem Lett. .

Abstract

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 GABA(B) 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.

PubMed Disclaimer

LinkOut - more resources