8-Methylureido-10-amino-10-methyl-imidazo[1,2- a ]indeno[1,2- e ]pyrazine-4-ones: Highly In vivo Potent and Selective AMPA Receptor Antagonists

Autor:	Jean-Marie Stutzmann, Marc Williams Debono, Alain Boireau, Arielle Genevois-Borella, Michel Cheve, Dominique Damour, Assunta Imperato, John Randle, Yves Ribeill, Jeremy Pratt, Serge Mignani, Patrick Jimonet, Marc Vuilhorgne, Georg Andrees Bohme
Rok vydání:	2000
Předmět:	Male Kainic acid Patch-Clamp Techniques Microinjections Pyrazine Stereochemistry Clinical Biochemistry Pharmaceutical Science Stereoisomerism AMPA receptor Biochemistry Chemical synthesis Mice Radioligand Assay chemistry.chemical_compound In vivo Drug Discovery Animals RNA Messenger Receptors AMPA alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Molecular Biology Brain Chemistry Cerebral Cortex Kainic Acid Molecular Structure Organic Chemistry Imidazoles Antagonist Biological activity Rats chemistry Pyrazines Oocytes Molecular Medicine Anticonvulsants
Zdroj:	Bioorganic & Medicinal Chemistry. 8:2211-2217
ISSN:	0968-0896
Popis:	Water soluble 8-methylureido-10-amino-10-methyl-imidazo[1,2-a]indeno[1,2-e]pyraz ine-4-one 4 represents a novel class of highly potent and selective AMPA receptors antagonists with in vivo activity. The dextrorotatory isomer (+)-4 was found to display the highest affinity with an IC50 of 10 nM. It also exhibited very good anticonvulsant effects after i.p., s.c. and i.v. administration in mice subjected to electrical convulsions (MES) and i.p. in audiogenic seizure-e in DBA/2 mice (ED50's < or = 10 mg/kg).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::675b2882dda673cbc94a2c3686682c41 https://doi.org/10.1016/s0968-0896(00)00161-9 Zobrazit plný text záznamu Full Text from ScienceDirect