Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor

Grove, Simon J .A. and Jamieson, Craig and Maclean, John K. F. and Morrow, John A. and Rankovic, Zoran (2010) Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. Journal of Medicinal Chemistry, 53 (20). pp. 7271-7279. ISSN 0022-2623 (https://doi.org/10.1021/jm1000419)

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Abstract

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.