Discovery of 2‑(2-Oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (Perampanel): A Novel, Noncompetitive α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropanoic Acid (AMPA) Receptor Antagonist

Dysfunction of glutamatergic neurotransmission has been implicated in the pathogenesis of epilepsy and numerous other neurological diseases. Here we describe the discovery of a series of 1,3,5-triaryl-1H-pyridin-2-one derivatives as noncompetitive antagonists of AMPA-type ionotropic glutamate recept...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-12, Vol.55 (23), p.10584-10600
Hauptverfasser:	Hibi, Shigeki, Ueno, Koshi, Nagato, Satoshi, Kawano, Koki, Ito, Koichi, Norimine, Yoshihiko, Takenaka, Osamu, Hanada, Takahisa, Yonaga, Masahiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological Availability Drug Discovery Half-Life High-Throughput Screening Assays In Vitro Techniques Magnetic Resonance Spectroscopy Male Mice Pyridones - chemistry Pyridones - pharmacokinetics Pyridones - pharmacology Rats Receptors, AMPA - antagonists & inhibitors Structure-Activity Relationship
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