Journal of Medicinal Chemistry · 2010 · 40 citations · 37 references
MedicineBiochemistryPharmacologyBiochemical PharmacologyMolecular PharmacologyStructure-activity RelationshipsAllosteric ModulationAllosteric RegulationLigand BindingReceptor PharmacologyReceptor RegulationReceptor-ligand InteractionsAllosteric AgonistsAllosteric Modulation Of G Protein-coupled ReceptorsAllosteric Modulation Of ReceptorsAllosteric Modulator BindingAllosteric Receptor PharmacologyPositive Allosteric ModulationPositive Allosteric ModulatorsReceptor Allosteric Sites
L-glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a fundamental role in the control of motor function, cognition and mood. The physiological effects of glutamate are mediated through two functionally distinct receptor families. While activation of metabotropic (G-protein coupled) glutamate receptors results in modulation of neuronal excitability and transmission, the ionotropic glutamate receptors (ligand-gated ion channels) are responsible for mediating the fast synaptic response to extracellular glutamate.
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The PyMOL Molecular Graphics System
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Structure of a glutamate-receptor ligand-binding core in complex with kainate
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