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Updated: Apr 11, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Co-operative binding assay for the characterization of mGlu4 allosteric modulators
Pekka Poutiainen1, Kun-Eek Kil1, Zhaoda Zhang1
1Athinoula A. Martinos Biomedical Imaging Center, Massachusetts General Hospital, Harvard Medical School, Boston, MA, USA.
Abstract:
The interest in the role of metabotropic glutamate receptor 4 (mGlu4) in CNS related disorders has increased the need for methods to investigate the binding of allosteric drug candidates. Our aim is to present the first fully characterized in vitro binding assay of mGlu4 positive allosteric modulators (PAMs). Results suggest that mGlu4 PAMs have characteristic co-operative binding with orthosteric glutamate, which offers a notable insight to the further development of mGlu4 targeted therapies.
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