Involuntary movements, or dyskinesia, represent a debilitating complication of levodopa (L-
dopa) therapy for Parkinson's disease (PD). L-dopa-induced dyskinesia (LID) are ultimately …

Allosteric modulation of GPCRs has initiated a new era of basic and translational discovery,
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …

Fragment screening of a thermostabilized mGlu5 receptor using a high-concentration
radioligand binding assay enabled the identification of moderate affinity, high ligand …

The condensation of 5-aminopyrazole with various bielectrophilic moieties results in the
formation of pyrazoloazines, an interesting array of fused heterocyclic systems. The …

In view of the fact that the G-protein-coupled receptors (GPCRs) sit at the top of the signaling
pathways triggering a diverse range of signaling cascades towards a cellular event, GPCRs …

Previous preclinical work has demonstrated the therapeutic potential of antagonists of the
group II metabotropic glutamate receptors (mGlus). Still, compounds that are selective for the …

Negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu5) have
potential for the treatment of psychiatric diseases including depression, fragile X syndrome …

Recently determined structures of class CG protein-coupled receptors (GPCRs) revealed the
location of allosteric binding sites and opened new opportunities for the discovery of novel …

Metabotropic glutamate receptors (mGluR) are predominantly involved in maintenance of
cellular homeostasis of central nervous system. However, evidences have suggested other …

Ketamine is a rapid-onset antidepressant whose efficacy long outlasts its pharmacokinetics.
Multiple studies suggest ketamine's antidepressant effects require increased α-amino-3 …