• Publications
  • Influence
Pharmacology and functions of metabotropic glutamate receptors.
  • P. Conn, J. Pin
  • Biology
    Annual review of pharmacology and toxicology
  • 1997
TLDR
The findings suggest that the mGluRs provide a novel target for development of therepeutic agents that could have a significant impact on neuropharmacology.
Metabotropic glutamate receptors: physiology, pharmacology, and disease.
TLDR
The widespread expression of mGluRs makes these receptors particularly attractive drug targets, and recent studies continue to validate the therapeutic utility of m GluR ligands in neurological and psychiatric disorders such as Alzheimer's disease, Parkinson's Disease, anxiety, depression, and schizophrenia.
Metabotropic Glutamate Receptors 1 and 5 Differentially Regulate CA1 Pyramidal Cell Function
TLDR
The use of two novel subtype-selective antagonists in experiments with whole-cell patch-clamp recording and Ca2+-imaging techniques revealed that each group I mGluR subtype plays distinct roles in regulating the function of CA1 pyramidal neurons.
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
TLDR
There have been tremendous advances in the discovery of novel ligands for GPCRs that act at allosteric sites to regulate receptor function that provide high selectivity, novel modes of efficacy and may lead to novel therapeutic agents for the treatment of multiple psychiatric and neurological human disorders.
A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral Models
TLDR
It is demonstrated that positive allosteric modulation of mGluR5 produces behavioral effects, suggesting that such modulation serves as a viable approach to increasing mGLUR5 activity in vivo.
Activation of Metabotropic Glutamate Receptor 5 Has Direct Excitatory Effects and Potentiates NMDA Receptor Currents in Neurons of the Subthalamic Nucleus
TLDR
It is reported that activation of group I metabotropic glutamate receptors (mGluRs) induces a direct excitation of STN neurons that is characterized by depolarization, increased firing frequency, and increased burst-firing activity, and the results suggest that mGluR5 may play an important role in the net excitatory drive to the STN from glutamatergic afferents.
Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment
TLDR
Evidence for in vivo behavioral effects of an allosteric potentiator of mGluRs is reported and it is suggested that potentiation ofmGluR4 may be a useful therapeutic approach to the treatment of PD.
A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors Has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity
TLDR
The finding that the effects of an orthosteric mGlu2/3 receptor agonist in these models can be mimicked by a selective allosteric potentiator of mGLU2 suggests that these effects are mediated by the mGlam2 receptor subtype.
Group III Metabotropic Glutamate Receptor-Mediated Modulation of the Striatopallidal Synapse
TLDR
It is found that intracerebroventricular injections of l-AP4 produce therapeutic benefit in both acute and chronic rodent models of Parkinson's disease, and the finding that mGluR4 may selectively modulate striatopallidal transmission raises the interesting possibility that activation of mGLUR4 could decrease the excessive inhibition of the GP that has been postulated to occur in Parkinson's Disease.
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