
Cell Reports | 杨巍/罗建红课题组揭示NMDA受体GluN2B磷酸化修 …
为此,研究人员运用 CRISPR-Cas9 技术构建了GluN2B Y1070F的遗传突变小鼠,采用系列行为学检测意外发现突变小鼠在基础水平及14天慢性束缚应激(Chronic restraint stress,CRS)暴露后均表现出显著抗抑郁样行为,而认知功能、焦虑、恐惧记忆、社交能力和探索等行为却没 ...
GluN2A and GluN2B NMDA receptors use distinct allosteric routes - Nature
2021年8月5日 · Here the authors show that GluN2A and GluN2B NMDA receptors — the two principal subtypes NMDARs in the adult CNS — operate through distinct long range allosteric mechanisms.
The differences between GluN2A and GluN2B signaling in the …
GluN2A and GluN2B are the main types of NMDA receptor subunit in the adult forebrain. Studies have demonstrated that they play different roles in a number of pathophysiological processes.
Recent progress in the development of GluN2B selective ligands
2023年6月2日 · Understanding of design rules and roles of GluN2B selective compounds will provide the link to medicinal chemists and neuroscientists to explore novel neurotherapeutic strategies against dysfunctions of glutamatergic neurotransmission.
Mol Psychiatry | 医学院石云团队揭示谷氨酸受体突变损害认知的新 …
2022年5月13日 · 在脑内,NMDA受体主要分为GluN2A和GluN2B两种类型。 这两种类型的NMDA受体在通道动力学上有所不同,GluN2A失活比GluN2B快,其介导的Ca2+信号可能相对较弱。 课题组在一个智力发育迟缓的儿童发现了GluN2A的一个罕见突变(K879R),即879位点的赖氨酸(K)突变成了精 ...
药渡Cyber解析杨森开发的GluN2B负别构调节剂分子设计和优化详 …
近日jmc报道了杨森公司以文献报道的选择性glun2b负别构调节剂为先导化合物,通过结构优化,改善adme和理化性质,得到具有高受体亲和力,良好的水溶性和体内靶标占有率的化合物31。
GluN2B-mediated regulation of silent synapses for receptor ...
GluN2B ablation reduces the proportion of silent synapses, but some of them can persist by substitution with GluN2C, which drives the aberrantly facilitated synaptic incorporation of calcium-impermeable AMPA-type glutamate receptors (AMPARs).
陆林课题组在《分子神经病学》发表文章,创新性提出了基 …
NMDA受体GluN2B亚基的选择性拮抗剂艾芬地尔也能产生快速抗抑郁作用,且没有成瘾性。 由此,陆林教授课题组提出了突触外DAPK1与NMDA受体2B亚基相互作用介导快速抗抑郁作用的新假说,这对于快速抗抑郁新药的研发具有重要的应用价值。
GluN2A and GluN2B subunit-containing NMDA receptors in …
Moreover, a GluN2B subunit-selective antagonist caused a greater reduction in Ca 2+ influx in those spines that supported a higher change in Ca 2+ per uncaging-evoked excitatory postsynaptic current (EPSC) which led the authors to conclude that GluN2B subunit-containing NMDARs support a greater Ca 2+ influx per unit of current .
杨巍/罗建红课题组Cell Reports发文揭示NMDA受体GluN2B磷酸化 …
2021年8月29日 · 为此, 研究人员运用CRISPR-Cas9技术构建了GluN2B Y1070F的遗传突变小鼠, 采用系列行为学检测意外发现突变小鼠在基础水平及14天慢性束缚应激(Chronic restraint stress,CRS)暴露后均表现出显著抗抑郁样行为,而认知功能、焦虑、恐惧记忆、社交能力和探 …