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XB-ART-47159
Bioorg Med Chem Lett 2013 Jul 01;2313:3901-4. doi: 10.1016/j.bmcl.2013.04.063.
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In vitro and in vivo evaluation of polymethylene tetraamine derivatives as NMDA receptor channel blockers.

Saiki R , Yoshizawa Y , Minarini A , Milelli A , Marchetti C , Tumiatti V , Toida T , Kashiwagi K , Igarashi K .


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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 (10mg/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.

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