• Corpus ID: 28004183

YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist.

@article{ShimizuSasamata1996YM90KPC,
  title={YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist.},
  author={Masao Shimizu‐Sasamata and Sachiko Kawasaki-Yatsugi and Masamichi Okada and Shuichi Sakamoto and S Yatsugi and Junji Togami and Ken-ichi Hatanaka and Junya Ohmori and Kazuo Koshiya and Shinji Usuda and Katsutoshi Murase},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1996},
  volume={276 1},
  pages={
          84-92
        }
}
We investigated the pharmacological properties and neuroprotective actions of a novel alpha-amino-3-hydroxy-5-methylisoxazole-y-propionate (AMPA)/kainate receptor antagonist, [6-(1H-imidazol-1-yl)-7-nitro-2,3-(1H,4H)-quinoxalinedione hydrochloride (YM90K); formerly YM900], in comparison with those of 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline (NBQX). YM90K selectively displaced [3H]-AMPA binding (Ki = 0.084 microM) and was less potent in inhibiting [3H]-kainate (Ki = 2.2 microM), [3H… 
YM872: a selective, potent and highly water-soluble alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist.
TLDR
The evidence for the neuroprotective efficacy of YM872 suggests its therapeutic potential in the treatment of acute stroke in humans and in rats and cats subjected to permanent occlusion of the left middle cerebral artery.
Functional Characterization of YM928, a Novel Noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist
TLDR
YM928 has potential as an oral therapeutic drug for various types of neurological disorders and had an anticonvulsant effect in sound-induced seizures in DBA/2 mice 45 min after oral administration at 3 mg/kg.
Effects of 2-[N-(4-Chlorophenyl)-N-methylamino]-4H-pyrido[3.2-e]-1,3-thiazin-4-one (YM928), an Orally Active α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptor Antagonist, in Models of Generalized Epileptic Seizure in Mice and Rats
TLDR
YM928 at doses of 2, 4, and 8 mg/kg p.o. did not significantly affect the threshold of electroshock seizure in rats after 16 days of repeated administration, indicating that YM 928 does not induce tolerance after subchronic administration.
SPD 502: a water-soluble and in vivo long-lasting AMPA antagonist with neuroprotective activity.
TLDR
In the in vitro and in vivo pharmacological properties of the novel glutamate antagonist SPD 502, SPD 502 resulted in a highly significant protection against the ischemia-induced damage in the hippocampal CA1 pyramidal neurons and increased the seizure threshold for electroshock-induced tonic seizures in mice.
Characterization of the renal tubular transport of zonampanel, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, by human organic anion transporters.
TLDR
It is suggested that the prototypical organic anion substrates (para-aminohippurate and estrone sulfate), cimetidine, probenecid, and zonampanel share binding specificity in each hOAT, whereas YM90K does not in hOat1, possibly due to it being the decarboxymethylated form.
Characterization of the binding site for a novel class of noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonists.
TLDR
Results indicate the existence of at least two physically distinct allosteric sites on the AMPA receptor through which channel activity or desensitization is modulated.
Non-N-methyl-D-aspartate (NMDA) receptor antagonist 1,2,3,4-tetrahydro-6-nitro-2,3-dioxo-benzo(f)quinoxaline-7-sulphonamide (NBQX) decreases functional disorders in cytotoxic brain oedema
TLDR
The results suggest that kainate/AMPA receptor channels are at least partially involved in the mechanism of brain damage induced by hexachlorophene, however, the polyamine binding site of the NMDA receptor evidently is not involved.
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