Synthesis and activity of spiroisoindolines as novel noncompetitive NMDA antagonists

Autor:	Linda M. Pullan, Clyde W. Draper, Jitendra Patel, Thomas M. Bare, Jitendra B. Patel, Charles D. McLaren
Rok vydání:	1993
Předmět:	Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Pharmacology Gerbil Biochemistry Affinities Neuroprotection nervous system In vivo Drug Discovery Molecular Medicine NMDA receptor Binding site Drug discrimination Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 3:55-60
ISSN:	0960-894X
Popis:	A series of novel spiroisoindolines was designed and synthesized as potential noncompetitive NMDA antagonists. Affinities of these compounds for the noncompetitive NMDA binding site were determined using [3H]TCP and found to possess IC50s ranging from 0.065 to 17μM. In vivo testing of 2′-methylspiro-[4,5,6,7-tetrahydrobenzothiophene-4,1′-(1,3-dihydroisoindole)] (43) showed it to antagonize NMDA-induced convulsions, to be neuroprotective in a gerbil model of ischemia, and not to generalize to MK-801 in a drug discrimination paradigm.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::a8986e12ad0581c7dce8e401b8ade4e5 https://doi.org/10.1016/s0960-894x(00)80091-8 Zobrazit plný text záznamu