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

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

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, in...

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Veröffentlicht in:Proceedings of the National Academy of Sciences - PNAS 2001-11, Vol.98 (23), p.13402
Hauptverfasser: Knoflach, Frederic, Mutel, Vincent, Jolidon, Synese, Kew, James N C
Format: Artikel
Sprache:eng
Schlagworte:
Amino acids
Biochemistry
Enzymes
Proteins
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Zusammenfassung: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.
ISSN:0027-8424
1091-6490