Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 16, Pages 6336-6347Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm5018913
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Funding
- University of Mississippi
- Purdue University
- Purdue Research Foundation
- Ralph W. and Grace M. Showalter Research Trust
- NIH National Center for Research Resources [C06 RR-14503-01]
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Since the discovery of the GABA(B) agonist and muscle relaxant badofen, there have been substantial advancements in the development of compounds that activate the GABAB receptor as agonists or positive allosteric modulators. For the agonists, most of the existing structure activity data apply to understanding the role of substituents on the backbone of GABA as well as replacing the carboxylic acid and amine groups. In the cases of the positive allosteric modulators, the allosteric binding site(s) and structure activity relationships are less well-defined; however, multiple classes of molecules have been discovered. The recent report of the X-ray structure of the GABAB receptor with bound agonists and antagonists provides new insights for the development of compounds that bind the orthosteric site of this receptor. From a therapeutic perspective, these data have enabled efforts in drug discovery in areas of addiction-related behavior, the treatment of anxiety, and the control of muscle contractility.
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