REL-1017是由Relmada Therapeutics研发的NMDA受体通道阻断剂。主要用于抑制一种被称为NMDA的神经递质的活动,该神经递质控制情绪。NMDA受体长期以来一直是抑郁症药物研发的目标,直接用药物阻断这个受体,就能像药物氯胺酮所产生的效果一样,可能比传统治疗更快缓解抑郁症状。REL-1017可以优先靶向过度活跃的GluN1-GluN2D NMDAR...
REL-1017是一种新化学实体(NCE),优先靶向过度活跃的GluN1-GluN2D NMDAR通道,有效阻止过量钙离子进入神经元内;同时还能够维持生理性谷氨酸神经传递,有利于恢复对心理健康至关重要的神经元回路。Relmada已围绕REL-1017建立了强大的知识产权保护体系,关键专利保护期延伸至2030年代中期。【单药治疗重度抑郁症!NMDA受体拮抗...
European Archives of Psychiatry and Clinical Neuroscience (2023) 273:1463–1476 https://doi.org/10.1007/s00406-023-01571-4 INVITED REVIEW Esmethadone‑HCl (REL‑1017): a promising rapid antidepressant Maurizio Fava1 · Stephen M. Stahl2,3 · Sara De Martin4 · Andrea...
作者: 药闻▶$Relmada治疗(RLMD)$公司宣布REL-1017作为单一疗法治疗重度抑郁症的3期RELIANCE III试验的结果:失败。
10月15日(路透社)-Relmada治疗公司:*RELMADA治疗公司-宣布REL-1017第2期研究的顶级结果,用于治疗难治性抑郁症*RELMA
REL-1017 has a higher preference for docking and undocking the open-channel conformation compared to ketamine. In conclusion, the pharmacological characteristics of REL-1017 at NMDARs, including relatively low affinity at the NMDAR, NR1-2D subtype preference in the presence of 1 mM Mg2+, tau ...
作者: #药闻简讯#$Relmada Therapeutics(RLMD)$停止 REL-1017 的 Reliance II 和 Relight 3 期研究
Objective: To test esmethadone (REL-1017) as adjunctive treatment in patients with major depressive disorder (MDD) and inadequate response to standard antidepressants. Methods: In this phase 3, double-blind, placebo-controlled trial, outpatients with MDD (DSM-5) were randomized to daily oral esme...
10 μM or 1 μM L-glutamate-induced currents were measured in the absence or presence of 10 μM REL-1017. Results 10 μM REL-1017 significantly reduced currents induced by 10 μM and 1 μM L-glutamate in NMDARs with the GluN2D subunit. Similarly, 10 μM REL-1017 significantly ...
Relmada Therapeutics, Inc. today announced that the U.S. Food and Drug Administration (FDA) has granted Fast Track designation to REL-1017.