|Description||NS-1209, an AMPA/GluR5 receptor antagonist, is a antiepileptic drug candidate currently under clinical trials.|
|Synonyms||2-[[5-[4-(dimethylsulfamoyl)phenyl]-8-methyl-2-oxo-7,9-dihydro-6H-pyrrolo[3,2-h]isoquinolin-3-yl]amino]oxy-4-hydroxybutanoic acid; NS-1209; NS 1209; NS1209; 245063-59-6; SPD-502; SPD502; SPD 502|
A poliamine amide as potent Spermidine uptake inhibitor.
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...
LY-326325, a decahydroisoquinaline derivative, has been found to be an AMPA receptor antagonist and was once studied for neuroprotection.
Aniracetam is a nootropics and neuroprotective drug.
IDRA-21, an analog of cyclothiazide, inhibits AMPA receptor desensitization and enhances cognition by a related mechanism. IDRA-21 inhibits synaptic and extrasy...
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...
4-Phenyl-2-pyrrolidone-1-acetamide is a GABA derivative that exhibited apparent immunocorrection properties during immunosuppression induced by cyclophosphamide...
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...
CMPDA is a positive allosteric modulator of AMPA receptors. Binds at the modulator binding pocket located at the interdimer interface and the clamshell hinges.
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...
2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor ag...
CP 465022, with anticonvulsant activity, is a potent, brain penetrant, orally active and selective noncompetitive AMPA receptor antagonist (IC50 = 25 nM in rat ...
Incubation of LY451395 with Actinoplanes missouriensis NRRL B3342 generated several metabolites that were previously detected in the in vivo metabolism studies ...
Farampator, also called as CX-691 or Org24448, is an AMPA receptor positive allosteric modulator and glycine reuptake inhibitor potentially for the treatment of...
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...
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...
Naspm 3HCl is a potent and selective Ca2+ permeable AMPA receptor blocker.
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 ...
Potent and selective AMPA antagonist.
The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses. At a concen...