Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
P Jeffrey Conn, A Christopoulos… - Nature reviews Drug …, 2009 - nature.com
Despite G-protein-coupled receptors (GPCRs) being among the most fruitful targets for
marketed drugs, intense discovery efforts for several GPCR subtypes have failed to deliver …
marketed drugs, intense discovery efforts for several GPCR subtypes have failed to deliver …
Pharmacology and functions of metabotropic glutamate receptors
▪ Abstract In the mid to late 1980s, studies were published that provided the first evidence
for the existence of glutamate receptors that are not ligand-gated cation channels but are …
for the existence of glutamate receptors that are not ligand-gated cation channels but are …
Metabotropic glutamate receptors: physiology, pharmacology, and disease
CM Niswender, PJ Conn - Annual review of pharmacology and …, 2010 - annualreviews.org
The metabotropic glutamate receptors (mGluRs) are family C G-protein-coupled receptors that
participate in the modulation of synaptic transmission and neuronal excitability throughout …
participate in the modulation of synaptic transmission and neuronal excitability throughout …
Metabotropic glutamate receptors in brain function and pathology
DD Schoepp, PJ Conn - Trends in Pharmacological Sciences, 1993 - cell.com
Metabotropic glutamate receptors (mGluRs) are a novel family of recently cloned G protein-coupled
receptors. These receptors are heterogeneous and coupled to multiple second …
receptors. These receptors are heterogeneous and coupled to multiple second …
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator
The excitatory neurotransmitter glutamate induces modulatory actions via the metabotropic
glutamate receptors (mGlus), which are class CG protein–coupled receptors (GPCRs). We …
glutamate receptors (mGlus), which are class CG protein–coupled receptors (GPCRs). We …
Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function
…, O Valenti, SF Traynelis, PJ Conn - Journal of …, 2001 - Soc Neuroscience
The activation of group I metabotropic glutamate receptors (mGluRs) produces a variety of
actions that lead to alterations in excitability and synaptic transmission in the CA1 region of …
actions that lead to alterations in excitability and synaptic transmission in the CA1 region of …
Activation of metabotropic glutamate receptor 5 has direct excitatory effects and potentiates NMDA receptor currents in neurons of the subthalamic nucleus
The subthalamic nucleus (STN) is a key nucleus in the basal ganglia motor circuit that
provides the major glutamatergic excitatory input to the basal ganglia output nuclei. The STN …
provides the major glutamatergic excitatory input to the basal ganglia output nuclei. The STN …
Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia
In recent years, the metabotropic glutamate (mGlu) receptors have emerged as potential
new drug targets for treatment of a range of CNS disorders. Some of the most compelling …
new drug targets for treatment of a range of CNS disorders. Some of the most compelling …
Metabotropic glutamate receptors in the basal ganglia motor circuit
PJ Conn, G Battaglia, MJ Marino… - Nature Reviews …, 2005 - nature.com
In recent years there have been tremendous advances in our understanding of the circuitry
of the basal ganglia and our ability to predict the behavioural effects of specific cellular …
of the basal ganglia and our ability to predict the behavioural effects of specific cellular …
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-d-aspartate receptor activity
…, DJ Pettibone, EM Scolnick, PJ Conn - Proceedings of the …, 2003 - National Acad Sciences
The molecular and neuronal substrates conferring on clozapine its unique and superior efficacy
in the treatment of schizophrenia remain elusive. The interaction of clozapine with many …
in the treatment of schizophrenia remain elusive. The interaction of clozapine with many …