4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with in vivo activity

Autor:	J M, Stutzmann, G A, Bohme, A, Boireau, D, Damour, M W, Debono, A, Genevois-Borella, A, Imperato, P, Jimonet, J, Pratt, J C, Randle, Y, Ribeill, M, Vuilhorgne, S, Mignani
Rok vydání:	2000
Předmět:	Drug Evaluation Preclinical Tetrazoles Isoquinolines Receptors N-Methyl-D-Aspartate Rats Inhibitory Concentration 50 Mice Structure-Activity Relationship Mice Inbred DBA Pyrazines Quinoxalines Animals Urea Anticonvulsants Receptors AMPA alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Zdroj:	Bioorganicmedicinal chemistry letters. 10(10)
ISSN:	0960-894X
Popis:	A novel series of 2-substituted-4,5-dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazine derivatives was synthesised. One of them, 4e-a highly water soluble compound exhibited a nanomolar affinity and demonstrated competitive antagonist properties at the ionotropic AMPA receptors. This compound also displayed potent anticonvulsant properties against electrically or sound-induced convulsions in mice after systemic administration, thus suggesting adequate brain penetration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::735ca79706c36ea211ad611ebf00595b https://pubmed.ncbi.nlm.nih.gov/10843235 Zobrazit plný text záznamu Full Text from ScienceDirect