Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers
摘要:
We have developed a new class of N-methyl-D-aspartate (NMDA) channel blockers having a conjugate structure that consists of a nitrogenous heterocyclic head and a tetraamine tail. Among them, dihydrodibenzazepine-homospermine conjugate (8) exhibited potent antagonistic activity at NR1/NR2A or NR1/NR2B NMDA subtype receptors compared with the lead compound, AQ343 (1), or memantine, as well as weak cytotoxicity. Its superior biological profiles compared with known compounds point to its potential use as therapeutic agents for neurological disorders. (c) 2007 Elsevier Ltd. All rights reserved.
COMPOUND HAVING ACTIVITY OF BLOCKING NMDA RECEPTOR CHANNEL, AND PHARMACEUTICAL AGENT USING THE SAME
申请人:National University Corporation Chiba University
公开号:EP2039354A1
公开(公告)日:2009-03-25
[PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound.
[MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.
COMPOUNDS BLOCKING THE NMDA RECEPTOR CHANNEL AND PHARMACEUTICAL AGENT USING THE SAME
申请人:National University Corporation Chiba University
公开号:EP2039354B1
公开(公告)日:2011-06-29
Compound Having Activity Of Blocking NMDA Receptor Channel, and Pharmaceutical Agent Using The Same
申请人:Igarashi Kazuei
公开号:US20090105223A1
公开(公告)日:2009-04-23
To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound.
A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (
1
), a salt thereof, or a hydrate of the compound or the salt.