Add to ORKGPositive allosteric modulators (PAMs) of metabotropic glutamate re-ceptor subtype5 (mGlu5) haveemergedasanexcitingnewapproach for the treatment of schizophrenia and other central nervous system (CNS) disorders. Of interest, some mGlu5 PAMs act as pure PAMs, only potentiating mGlu5 responses to glutamate whereas others [al-losteric agonists coupled with PAM activity (ago-PAMs)] potentiate responses to glutamate and have intrinsic allosteric agonist activity in mGlu5-expressing cell lines. All mGlu5 PAMs previously shown to have efficacy in animal models act as ago-PAMs in cell lines, raising the possibility that allosteric agonist activity is critical for in vivo effi-cacy. We have now optimized novel mGlu5 pure PAMs that are devoid of detec...
International audienceExciting advances have been made in the discovery of selective positive allost...
International audienceExciting advances have been made in the discovery of selective positive allost...
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets ...
Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (C...
Metabotropic glutamate (mGlu) receptors are considered as candidate drug targets for the treatment o...
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu<sub>5</sub>) repres...
Metabotropic glutamate receptors belong to class C G-protein-coupled receptors and consist of eight ...
abstract: Studies utilizing selective pharmacological antagonists or targeted gene deletion have dem...
The therapeutic potential of selective mGlu<sub>1</sub> activation is vastly unexplored relative to ...
The therapeutic potential of selective mGlu<sub>1</sub> activation is vastly unexplored relative to ...
Metabotropic glutamate receptors (mGluR) belong to the G-protein-coupled receptor (GPCR) family and ...
Drug discovery programs increasingly are focusing on allosteric modulators as ameans tomodify the ac...
In schizophrenia, mGlu5 receptor hypofunction has been linked with neuropathology and cognitive defi...
Selective potentiators of glutamate response at metabotropic glutamate receptor subtype 5 (mGluR5) h...
As part of our ongoing small-molecule metabotropic glutamate (mGlu) receptor positive allosteric mod...
International audienceExciting advances have been made in the discovery of selective positive allost...
International audienceExciting advances have been made in the discovery of selective positive allost...
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets ...
Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (C...
Metabotropic glutamate (mGlu) receptors are considered as candidate drug targets for the treatment o...
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu<sub>5</sub>) repres...
Metabotropic glutamate receptors belong to class C G-protein-coupled receptors and consist of eight ...
abstract: Studies utilizing selective pharmacological antagonists or targeted gene deletion have dem...
The therapeutic potential of selective mGlu<sub>1</sub> activation is vastly unexplored relative to ...
The therapeutic potential of selective mGlu<sub>1</sub> activation is vastly unexplored relative to ...
Metabotropic glutamate receptors (mGluR) belong to the G-protein-coupled receptor (GPCR) family and ...
Drug discovery programs increasingly are focusing on allosteric modulators as ameans tomodify the ac...
In schizophrenia, mGlu5 receptor hypofunction has been linked with neuropathology and cognitive defi...
Selective potentiators of glutamate response at metabotropic glutamate receptor subtype 5 (mGluR5) h...
As part of our ongoing small-molecule metabotropic glutamate (mGlu) receptor positive allosteric mod...
International audienceExciting advances have been made in the discovery of selective positive allost...
International audienceExciting advances have been made in the discovery of selective positive allost...
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets ...