Design and synthesis of a novel water-soluble NMDA receptor antagonist with a 1,4,7,10-tetraazacyclododecane group.
Design and synthesis of a novel water-soluble NMDA receptor antagonist with a 1,4,7,10-tetraazacyclododecane group.
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设计和合成具有 1,4,7,10-四氮杂环十二烷基团的新型水溶性 NMDA 受体拮抗剂。
DOI：
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发表时间：
2005
影响因子：
1.7
通讯作者：
Muneharu Miyake
中科院分区：
文献类型：
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作者：
T. Masuko;K. Metori;Y. Kizawa;T. Kusama;Muneharu Miyake
多胺，特别是精胺，抑制N-甲基-D-天冬氨酸（NMDA）受体作为开放通道阻滞剂。合成了两种含1，4，7，10-四氮杂环十二烷环多胺的水溶性NMDA受体拮抗剂ACCn（1）和TGCn（2），并利用爪蟾卵母细胞表达的重组NMDA受体的电压钳记录研究了这两种化合物对NMDA受体的作用。这些化合物在-70 mV电压钳制下抑制卵母细胞中NR 1/NR 2A和NR 1/NR 2B受体亚型的宏观电流。化合物对NR 1/NR 2A受体的抑制作用比NR 1/NR 2B受体的抑制作用更明显。ACCn（1）对两种NMDA受体的抑制作用均强于TGCn（2）。
Polyamines, especially spermine, inhibit N-methyl-D-aspartate (NMDA) receptors as open channel blockers. Two types of water-soluble NMDA receptor antagonist, ACCn (1) and TGCn (2), with a 1,4,7,10-tetraazacyclododecane cyclic polyamine group, were synthesized and the effects of both compounds on NMDA receptors were studied using voltage-clamp recordings of recombinant NMDA receptors expressed in Xenopus oocytes. These compounds inhibited macroscopic currents in both NR1/NR2A and NR1/NR2B receptor subtypes in oocytes voltage-clamped at -70 mV. Inhibition by the compounds of NR1/NR2A receptors were more prominent than that of NR1/NR2B receptors. The inhibitory effects of ACCn (1) on both NMDA receptors were more potent than those of TGCn (2).
影响因子：
3.6
作者：
Masuko, T;Kashiwagi, K;Williams, K
通讯作者：
Williams, K