|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|
GYKI-53784, a dioxolbenzene derivative, has been found to be a AMPA receptor antagonist that could block excitotoxicity and decrease auditory nerve activity at ...
NS-1209, an AMPA/GluR5 receptor antagonist, is a antiepileptic drug candidate currently under clinical trials.
4-Phenyl-2-pyrrolidone-1-acetamide is a GABA derivative that exhibited apparent immunocorrection properties during immunosuppression induced by cyclophosphamide...
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...
Org-26576 is a positive allosteric modulator of AMPA receptor. Org-26576 increases the anteroventral and laterodorsal thalamus, cingulate cortex, dentate gyrus ...
(S)-(-)-5-Fluorowillardiine Hcl is a potent and specific AMPAR agonist.
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...
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 ...
Naspm 3HCl is a potent and selective Ca2+ permeable AMPA receptor blocker.
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...
CP 465022, with anticonvulsant activity, is a potent, brain penetrant, orally active and selective noncompetitive AMPA receptor antagonist (IC50 = 25 nM in rat ...
Noopept is a nootropic and neuroprotective drug that normalizes the balance of the pro- and antioxidant systems. Noopept modulates a variety of physiological fu...
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-53405 is a noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) antagonist. It can bind to Xenopus brain membranes ...
CX516 is a positive allosteric modulator at AMPA receptor that inhibits the deactivation of AMPA receptors. CX-516 is a nootropic and ampakine agent.
Incubation of LY451395 with Actinoplanes missouriensis NRRL B3342 generated several metabolites that were previously detected in the in vivo metabolism studies ...
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...
2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor ag...
LY-326325, a decahydroisoquinaline derivative, has been found to be an AMPA receptor antagonist and was once studied for neuroprotection.
Farampator, also called as CX-691 or Org24448, is an AMPA receptor positive allosteric modulator and glycine reuptake inhibitor potentially for the treatment of...