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2917551-59-6
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AMPA receptor modulator-4
CAS No. : 2917551-59-6
MCE 国际站：AMPA receptor modulator-4
产品活性：AMPA receptor modulator-4 是一种 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD)，是口服有效的 AMPA 受体 (AMPAR PAM) 的正变构调节剂。AMPA receptor modulator-4 可以透过血脑屏障。AMPA receptor modulator-4 可提高小鼠的认知能力并改善工作记忆能力。
研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：iGluR
In Vitro: AMPA receptor modulator-4 (compound 15e) has pEC50 of 5.66 on the calcium influx induced by 1 mM Glutamate on HEK293 cells stably expressing the GluA2(Q) subunit.
AMPA receptor modulator-4 has EC2x=2.1 μM (FlipR)-1.5 μM (FDSS) .
In Vivo: AMPA receptor modulator-4 (compound 15e; 10 and 30 mg/kg; IP; once) increases the duration of the LTP at a dose of 10 mg/kg in rats.
AMPA receptor modulator-4 (1 and 3 mg/kg; po) 1 h before the three sessions significantly increases the cognition performance of CD1 mice.
AMPA receptor modulator-4 (0.03, 0.1 and 0.3 mg/kg; ip) improves the performance of spontaneous alternation and improves working memory performance in C57BI/6 mice.
AMPA receptor modulator-4 (30, 100 mg/kg; po; once) has non-pro-convulsant effect in NMRI mice.
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文献和实验Monitoring Synaptic Plasticity by Imaging AMPA Receptor Content and Dynamics on Dendritic Spines
brain structures that are beyond the reach of traditional microscopes. Here, we describe an AMPA receptor-based optical approach to monitor recent history of synaptic plasticity. This method allows the identification of spines that have recently acquired
to LTD. These signaling molecules influence synaptic strength by modifying the phosphorylation state of many target proteins. In particular, bi-directional alterations in the phosphorylation of AMPA receptors can affect the trafficking and conductance of these receptors
Methods for Evaluation of Positive Allosteric Modulators of Glutamate AMPA Receptors
and are intimately involved in long-term changes in synaptic plasticity thought to underlie mnemonic processing. By definition, positive allosteric modulators do not affect AMPA receptor activity alone but can markedly enhance ion flux through the ion channel pore
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