ChemInform Abstract: Pyrrolylquinoxalinediones: Dicarboxylates as Highly Potent AMPA Receptor Antagonists

Autor:	H. P. Hofmann, B. Behl, H. J. Teschendorf, W. Lubisch
Rok vydání:	2010
Předmět:	chemistry.chemical_compound Maximal electroshock nervous system chemistry In vivo musculoskeletal neural and ocular physiology Glutamate receptor General Medicine AMPA receptor Pharmacology Selectivity AMPA Receptor Antagonists Pyrrole
Zdroj:	ChemInform. 29
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.199804242
Popis:	Pyrrolylquinoxalinediones carrying carboxylates at the pyrrole side-chain were synthesized and evaluated for AMPA receptor binding and for selectivity over other glutamate receptors. Particularly dicarboxy derivatives represent selective and highly potent AMPA antagonists. Moreover, several compounds displayed a remarkable efficacy against AMPA induced lethal convulsions and maximal electroshock seizures (MES) in mice. The good in vivo efficacy of the highly polar compounds suggests the involvement of an active transport mechanism.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::a78058e56032d8f24a6ed7c14e98d7ae https://doi.org/10.1002/chin.199804242 Zobrazit plný text záznamu Plný text