期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 13, 页码 3901-3904出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.04.063
关键词
Polymethylene teraamine derivative; NMDA receptor channel blocker
资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan
- MIUR, Rome [PRIN 2009ESXPT2_001]
- Grants-in-Aid for Scientific Research [23390038] Funding Source: KAKEN
The biological activities of six symmetrically substituted 2-methoxy-benzyl polymethylene tetraamines (1-4) and diphenylethyl polymethylene tetraamines (5 and 6) as N-methyl-D-aspartate (NMDA) receptor channel blockers, were evaluated in vitro and in vivo. Although all compounds exhibited stronger channel block activities in comparison to memantine in Xenopus oocytes voltage clamped at -70 mV, only compound 2 (0.4 mg/kg intravenous injection) decreased the size of brain infarction in a photochemically induced thrombosis model mice at the same extent of memantine (10 mg/kg intravenous injection). Other compounds (1, 3, 4, 5 and 6) did not decrease the size of brain infarction significantly due to the limited injection doses. The present study suggests that compound 2 could represent a valuable lead compound to design low toxicity polyamines for clinical use against stroke. (c) 2013 Elsevier Ltd. All rights reserved.
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