117928-94-6 Usage
Uses
Different sources of media describe the Uses of 117928-94-6 differently. You can refer to the following data:
1. Rapastinel is a novel antidepressant drug approved as an adjunctive therapy for the treatment of treatment-resistant major depressive disorder. It is a centrally active, intravenously administered (non-orally active) amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) that acts as a selective, weak partial agonist (mixed antagonist/agonist) of an allosteric site at the glycine site of the NMDA receptor complex (Emax ≈ 25%).The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to both inhibit and enhance NMDA receptor-mediated signal transduction.
2. GLYX-13 is a long lasting and rapid acting antidepressant. Investigational drug for the treatment of depressive disoder.
3. GLYX-13 trifluoroacetate has been used as an activator of NMDA (N-methyl-D-aspartate) receptor.
Biochem/physiol Actions
GLYX-13 is a glycine-site functional partial agonist (GFPA) selective modulator of the NMDA receptor (NMDAR). It is a brain penetrable tetrapeptide which acts as a positive allosteric modulator of the NMDA receptor, acting via the glycine site. GLYX-13 has been found to be a cognitive enhancer in learning models and is currently in clinical trials as an antidepressant.
Check Digit Verification of cas no
The CAS Registry Mumber 117928-94-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,7,9,2 and 8 respectively; the second part has 2 digits, 9 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 117928-94:
(8*1)+(7*1)+(6*7)+(5*9)+(4*2)+(3*8)+(2*9)+(1*4)=156
156 % 10 = 6
So 117928-94-6 is a valid CAS Registry Number.
117928-94-6Relevant articles and documents
Scale-Up synthesis and identification of GLYX-13, a NMDAR glycine-site partial agonist for the treatment of major depressive disorder
Li, Wenchao,Liu, Jingjian,Fan, Minghua,Li, Zhongtang,Chen, Yin,Zhang, Guisen,Huang, Zhuo,Zhang, Liangren
, (2018)
GLYX-13, a NMDAR glycine-site partial agonist, was discovered as a promising antidepressant with rapidly acting effects but no ketamine-like side effects. However, the reported synthetic process route had deficiencies of low yield and the use of unfriendly reagents. Here, we report a scaled-up synthesis of GLYX-13 with an overall yield of 30% on the hectogram scale with a column chromatography-free strategy, where the coupling and deprotection reaction conditions were systematically optimized. Meanwhile, the absolute configuration of precursor compound of GLYX-13 was identified by X-ray single crystal diffraction. Finally, the activity of GLYX-13 was verified in the cortical neurons of mice through whole-cell voltage-clamp technique.
PROCESS AND INTERMEDIATES FOR SYNTHESIS OF PEPTIDE COMPOUNDS
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, (2019/02/13)
Disclosed is a new process and intermediates for preparing dipyrrolidine peptide compounds such as, for example, rapastinel. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.
