|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.|
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...
CP 465022, with anticonvulsant activity, is a potent, brain penetrant, orally active and selective noncompetitive AMPA receptor antagonist (IC50 = 25 nM in rat ...
A poliamine amide as potent Spermidine uptake inhibitor.
4-Phenyl-2-pyrrolidone-1-acetamide is a GABA derivative that exhibited apparent immunocorrection properties during immunosuppression induced by cyclophosphamide...
The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses. At a concen...
Incubation of LY451395 with Actinoplanes missouriensis NRRL B3342 generated several metabolites that were previously detected in the in vivo metabolism studies ...
LY-326325, a decahydroisoquinaline derivative, has been found to be an AMPA receptor antagonist and was once studied for neuroprotection.
Talampanel, also known as LY300164 and GYKI-53773, is a glutamate receptor inhibitor with anti-seizure activity. Talampanel is also an orally active, potent an...
(S)-(-)-5-Fluorowillardiine Hcl is a potent and specific AMPAR agonist.
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...
A more potent and selective AMPA receptor agonist (at hGluR1 and hGluR2) than AMPA itself (Ki = 14.7, 25.1, and 1820 nM for hGluR1, hGluR2 and hGluR5 respective...
AMPA receptors mediate most of the excitatory neurotransmission and play a key role in synaptic plasticity in the mammalian central nervous system (CNS). Recent...
CMPDA is a positive allosteric modulator of AMPA receptors. Binds at the modulator binding pocket located at the interdimer interface and the clamshell hinges.
CX516 is a positive allosteric modulator at AMPA receptor that inhibits the deactivation of AMPA receptors. CX-516 is a nootropic and ampakine agent.
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 ...
Potent and selective AMPA antagonist.
ZK200775 hydrate(Fanapanel; MPQX) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 &mu...
GYKI-53784, a dioxolbenzene derivative, has been found to be a AMPA receptor antagonist that could block excitotoxicity and decrease auditory nerve activity at ...
GYKI-52466 is a non-competitive AMPA receptor antagonist. It belongs to 2,3-benzodiazepine that acts as an ionotropic glutamate receptor antagonist. It has anti...
EGIS-8332 potently decreased AMPA and quisqualate induced LDH release (IC50 = 5.2 ± 0.4 and 7.4 ± 1.3 μM, respectively) from the cells. The inhibition of the AM...