|Description||The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses. At a concentration of 1.8 mM, Ca2+ inhibited the currents induced by 100 microM willardiine by approximately 50%. In newborn mice (P5, histopathology at P10), local injection of the AMPA receptor agonist S-bromo-willardiine at day 5 after birth induced cortical damage and white matter damage, which was reduced in a dose-dependent manner by the AMPA receptor antagonists.|
CP 465022, with anticonvulsant activity, is a potent, brain penetrant, orally active and selective noncompetitive AMPA receptor antagonist (IC50 = 25 nM in rat ...
It is one of a series of AMPA modulators for the potential treatment of Alzheimer's disease, schizophrenia, and mild cognitive impairment (MCI). An ampakine dru...
NS-1209, an AMPA/GluR5 receptor antagonist, is a antiepileptic drug candidate currently under clinical trials.
GYKI-53784, a dioxolbenzene derivative, has been found to be a AMPA receptor antagonist that could block excitotoxicity and decrease auditory nerve activity at ...
IDRA-21, an analog of cyclothiazide, inhibits AMPA receptor desensitization and enhances cognition by a related mechanism. IDRA-21 inhibits synaptic and extrasy...
GYKI-53405 is a noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) antagonist. It can bind to Xenopus brain membranes ...
Aniracetam is a nootropics and neuroprotective drug.
GYKI-47261 is a non-competitive AMPA receptor antagonist (IC50 = 2.5 μM) and a CYP2E1 inducer. GYKI-47261 shows broad spectrum anticonvulsive activity and neuro...
Competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [3H]-AMPA (Ki = 120 nM) and [3H]-CNQX (Ki = 32 nM) binding sites and ...
This active molecular is an AMPA receptor antagonist which blocks AMPA receptors in 10-20µM concentrations. It is also a Glutamate receptor antagonist. NBQX was...
CMPDA is a positive allosteric modulator of AMPA receptors. Binds at the modulator binding pocket located at the interdimer interface and the clamshell hinges.
2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor ag...
Potent and selective AMPA antagonist.
Naspm 3HCl is a potent and selective Ca2+ permeable AMPA receptor blocker.
A poliamine amide as potent Spermidine uptake inhibitor.
AMPA receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian central nervous system (CNS). Recent...
4-Phenyl-2-pyrrolidone-1-acetamide is a GABA derivative that exhibited apparent immunocorrection properties during immunosuppression induced by cyclophosphamide...
Tezampanel, a decahydroisoquinoline derivative, has been found to be AMPA receptor as well as Kainic acid receptor antagonist that could probably be useful in s...
GYKI 47261 dihydrochloride
This active molecular is Non-competitiv a AMPA antagonist with IC50 value of 2.5 μM. GYKI-47261 is also a CYP2E1 inducer. GYKI-47261 showed broad spectrum of an...
LY3130481, a benzothiazol derivative, has been found to be the first AMPA receptor antagonist that could be probably effective in studies of epilepsy. It has ju...