NDLI: Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site

Content Provider	PubMed Central
Author	Frédéric, Knoflach Vincent, Mutel Jolidon, Synèse Kew, James N. C. Malherbe, Pari Vieira, Eric Wichmann, Jürgen Kemp, John A.
Copyright Year	2001
Abstract	We have identified two chemical series of compounds acting as selective positive allosteric modulators (enhancers) of native and recombinant metabotropic glutamate 1 (mGlu1) receptors. These compounds did not directly activate mGlu1 receptors but markedly potentiated agonist-stimulated responses, increasing potency and maximum efficacy. Binding of these compounds increased the affinity of a radiolabeled glutamate-site agonist at its extracellular N-terminal binding site. Chimeric and mutated receptors were used to localize amino acids in the receptor transmembrane region critical for these enhancing properties. Finally, the compounds potentiated synaptically evoked mGlu1 receptor responses in rat brain slices. The discovery of selective positive allosteric modulators of mGlu1 receptors opens up the possibility to develop a similar class of compounds for other family 3 G protein-coupled receptors.
Related Links	http://dx.doi.org/10.1073/pnas.231358298
Ending Page	13407
Page Count	6
Starting Page	13402
File Format	PDF
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	23
Volume Number	98
Language	English
Publisher	The National Academy of Sciences
Publisher Date	2001-11-06
Access Restriction	Open
Rights Holder	The National Academy of Sciences
Subject Keyword	General Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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