|Description||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 anticonvulsive and really good neuroprotective effect in vivo. AMPA and NMDA receptors have been implicated in the regulation of corticostriatal synaptic efficacy which abundantly expressed on striatal medium spiny neurons. In 2000, preclinical development for Epilepsy in Hungar was on-going, but no development was reported yet.|
|Synonyms||4-(8-chloro-2-methyl-11H-imidazo[1,2-c][2,3]benzodiazepin-6-yl)aniline;dihydrochloride;220445-20-5 (free base)|
|Solubility||Soluble to 100 mM in DMSO|
|Application||Epilepsy; Parkinson's disease; Stroke|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Current Developer||Originator: IVAX Pharmaceuticals UK; Nonindustrial source|
NBQX disodium salt
The sodium salt form of NBQX, which has been found to be an AMPA receptor antagonist and could be used as neuroprotective as well as anticonvulsant agent.
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...
CX516 is a positive allosteric modulator at AMPA receptor that inhibits the deactivation of AMPA receptors. CX-516 is a nootropic and ampakine agent.
YM 90K hydrochloride
YM 90K hydrochloride is a selective AMPA receptor antagonist (Ki = 84, 2200 and > 37000 nM for AMPA, kainate and NMDA receptors, respectively). YM 90K hydrochlo...
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 ...
Farampator, also called as CX-691 or Org24448, is an AMPA receptor positive allosteric modulator and glycine reuptake inhibitor potentially for the treatment of...
(S)-AMPA is an active enantiomer of AMPA, which has been found to be a definitive agonist of the AMPA glutamatergic ionotropic receptor.
Kynurenic acid is a product of L-Tryptophan metabolism. It is a non-selective antagonist at NMDA and AMPA/kainate receptors. It could block kainic acid neurotox...
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...
PF 06409577 is a potent and selective allosteric activator of AMPK (EC50 values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively) for the potenti...
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...
A poliamine amide as potent Spermidine uptake inhibitor.
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...
The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses. At a concen...
IEM 1460, an adamantane derivative, is a selective and voltage-dependent open-channel antagonist of AMPA receptors. It is Ca2+ permeable and lacks GluR2 subunit...
4-Phenyl-2-pyrrolidone-1-acetamide is a GABA derivative that exhibited apparent immunocorrection properties during immunosuppression induced by cyclophosphamide...
(S)-CPW 399 has been found to be a subtype-selective weakly desensitising AMPA agonist.
Aniracetam is a nootropics and neuroprotective drug.
S 18986 is a positive allosteric modulator of AMPA receptors that enhances (S)-AMPA-mediated noradrenaline release in rat hippocampal and frontal cortex slices....
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...