Perampanel is an aryl substituted 2-pyridone AMPA receptor antagonist that was recently approved as a treatment for epilepsy. The drug potently inhibits AMPA receptor responses but the mode of block has not been characterized. Here the action of perampanel on AMPA receptors was investigated by whole-cell voltage-clamp recording in cultured rat hippocampal neurons. Perampanel caused a slow (τ∼1 ...

The delivery of neurotransmitter receptors into synapses is essential for synaptic function and plasticity. In particular, AMPA-type glutamate receptors (AMPA receptors) reach excitatory synapses according to two distinct routes: a regulated pathway, which operates transiently during synaptic plasticity, and a constitutive pathway, which maintains synaptic function under conditions of basal tra...

Microinjection of S-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) in the nucleus of the solitary tract (NTS) of conscious rats causes hypertension, bradycardia, and vasoconstriction in the renal, mesenteric, and hindquarter vascular beds. In the hindquarter, the initial vasoconstriction is followed by vasodilation with AMPA doses >5 pmol/100 nl. To test the hypothesis that thi...

Although cultured astrocytes express functional glutamate receptors, they are generally resistant to excitotoxic cell death. We explored the role of receptor desensitization in glutamate-mediated astrocyte injury. In cultures of type 1 astrocytes from mouse neocortex, brief application of AMPA evoked small, rapidly desensitizing inward currents, whereas kainate evoked small, sustained currents....

Aminomethylphosphonic acid (AMPA) is formed in glyphosate-treated glyphosate-resistant (GR) and glyphosate-sensitive (GS) soybean [Glycine max (L.) Merr.] plants and is known to cause yellowing in soybean. Although, AMPA is less phytotoxic than glyphosate, its mode of action is different from that of glyphosate and is still unknown. Greenhouse studies were conducted at Stoneville, MS to determi...

The functional properties of alpha-amino-3-hydroxy-5-methy-4-isoxazole propionate (AMPA) receptors in different brain regions, such as hippocampus and cerebellum, have been well studied in vitro and in vivo. The AMPA receptors present a unique characteristic in the mechanisms of subunit regulation during LTP (long-term potentiation) and LTD (long-term depression), which are involved in the traf...

Overactivation of ionotropic glutamate receptors has been implicated in the pathophysiology of traumatic brain injury. Using an in vitro cell injury model, we examined the effects of stretch-induced traumatic injury on the AMPA subtype of ionotropic glutamate receptors in cultured neonatal cortical neurons. Recordings made using the whole-cell patch-clamp technique revealed that a subpopulation...

The effects of potassium thiocyanate on the binding of DL-aamino-3-hydroxy-5-methylisoxazolepropionic acid (AMPA), 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), and L-glutamate to the AMPA receptor complex were studied in rat brain membranes. Thiocyanate increased the affinity of AMPA receptors for both AMPA and i.-glutamate and decreased the affinity for CNQX. Displacement of [3H]CNQX binding b...

AMPA receptors mediate fast synaptic transmission at excitatory synapses in the CNS and are crucial during neuronal development, synaptic plasticity and structural remodeling. AMPA receptors lacking GluR2 subunits are permeable to Ca(2+) and Zn(2+). Ca(2+) permeation through AMPA receptors is crucial in several forms of synaptic plasticity and cell death associated with neurological diseases an...

In this work we study the excitatory AMPA, and NMDA, and inhibitory GABAA receptor mediated dynamical changes in neuronal networks of neonatal rat cortex in vitro. Extracellular network-wide activity was recorded with 59 planar electrodes simultaneously under different pharmacological conditions. We analyzed the changes of overall network activity and network-wide burst frequency between baseli...