Glutamate receptor ion channels

ML Mayer - Current opinion in neurobiology, 2005 - Elsevier
Glutamate receptor ion channels mediate excitatory responses at the majority of CNS
synapses. They are the only ligand-gated ion channels for which multiple high-resolution …

Pharmacology of ampakine modulators: from AMPA receptors to synapses and behavior

AC Arai, M Kessler - Current drug targets, 2007 - ingentaconnect.com
Ampakines are drugs structurally derived from aniracetam that potentiate currents mediated
by AMPA type glutamate receptors. These drugs slow deactivation and attenuate …

Mechanism of positive allosteric modulators acting on AMPA receptors

R Jin, S Clark, AM Weeks, JT Dudman… - Journal of …, 2005 - Soc Neuroscience
Ligand-gated ion channels involved in the modulation of synaptic strength are the AMPA,
kainate, and NMDA glutamate receptors. Small molecules that potentiate AMPA receptor …

Kynurenic acid has a dual action on AMPA receptor responses

C Prescott, AM Weeks, KJ Staley, KM Partin - Neuroscience letters, 2006 - Elsevier
Glutamate is the predominant excitatory neurotransmitter in the central nervous system. The
receptors that bind glutamate, including N-methyl-d-aspartate (NMDA) and α-amino-3 …

AMPA receptor modulators as cognitive enhancers

G Lynch - Current opinion in pharmacology, 2004 - Elsevier
AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid)-type glutamate receptors
mediate fast excitatory transmission throughout the central nervous system. Positive …

Different domains of the AMPA receptor direct stargazin-mediated trafficking and stargazin-mediated modulation of kinetics

MA Bedoukian, AM Weeks, KM Partin - Journal of Biological Chemistry, 2006 - ASBMB
Stargazin is an accessory protein of AMPA receptors that enhances surface expression and
also affects the biophysical properties of the receptor. AMPA receptor domains necessary for …

Challenges for and current status of research into positive modulators of AMPA receptors

SE Ward, BD Bax, M Harries - British journal of pharmacology, 2010 - Wiley Online Library
AMPA receptors consist of a family of hetero‐oligomeric (tetrameric) receptors arising from
four genes, each of which encodes a distinct receptor subunit (GluA1‐4). Recombinant …

Structural basis for positive allosteric modulation of AMPA and kainate receptors

K Frydenvang, DS Pickering… - The Journal of …, 2022 - Wiley Online Library
This paper summarizes the present knowledge on how positive allosteric modulators
(PAMs) interact with the ligand‐binding domain (LBD) of AMPA and kainate receptors …

Effects of the lurcher mutation on GluR1 desensitization and activation kinetics

RM Klein, JR Howe - Journal of Neuroscience, 2004 - Soc Neuroscience
Previous studies of the lurcher mutation in GluR1 channels concluded that its main effect is
to create constitutively active channels (;). GluR1Lc channels also exhibit slowed kinetics …

Discovery of N-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a Novel Clinical AMPA Receptor Positive Modulator

SE Ward, M Harries, L Aldegheri… - Journal of medicinal …, 2010 - ACS Publications
A series of AMPA receptor positive allosteric modulators has been optimized from poorly
penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS …