In‐vitro Characterization of YM872, a Selective, Potent and Highly Water‐soluble α‐Amino‐3‐hydroxy‐5‐methylisoxazole‐4‐propionate Receptor Antagonist

@article{Kohara1998InvitroCO,
  title={In‐vitro Characterization of YM872, a Selective, Potent and Highly Water‐soluble $\alpha$‐Amino‐3‐hydroxy‐5‐methylisoxazole‐4‐propionate Receptor Antagonist},
  author={Atsuyuki Kohara and Masamichi Okada and Rie Tsutsumi and Kazushige Ohno and Masayasu Takahashi and Masao Shimizu‐Sasamata and Jun-ichi Shishikura and Hiroshi Inami and Shuichi Sakamoto and Tokio Yamaguchi},
  journal={Journal of Pharmacy and Pharmacology},
  year={1998},
  volume={50}
}
The in‐vitro pharmacological properties of (2,3‐dioxo‐7‐(1H‐imidazol‐***1‐yl)‐6‐nitro‐1,2,3,4‐tetrahydro‐1‐quinoxalinyl)‐acetic acid monohydrate, YM872, a novel and highly water‐soluble α‐amino‐3‐hydroxy‐5‐methylisoxazole‐4‐propionate (AMPA)‐receptor antagonist were investigated. 
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.
Competitive AMPA receptor antagonists
TLDR
The present review reports the history of competitive AMPA receptor antagonists from 1988 up to today, providing a systematic coverage of both the open and patent literature.
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.
Synergistic analgesic effects of intrathecal midazolam and NMDA or AMPA receptor antagonists in rats
TLDR
Results suggest a functional coupling of benzodiazepine—aminobutyric acid (GABA)A receptor with NMDA and AMPA receptors in acute and persistent inflammatory nociceptive mechanisms in the spinal cord.
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TLDR
Evidence for the neuroprotective efficacy of YM872 suggests its therapeutic potential in the treatment of acute stroke in humans and supports the notion that the AMPA receptor plays an important role in the progression of focal ischemic damage in a gyrencephalic model.
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TLDR
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TLDR
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