117928-94-6 Usage
Description
GLYX 13, also known as Rapastinel, is an investigational drug developed as a novel antidepressant for the treatment of depressive disorders, particularly major depressive disorder. It is a centrally active, intravenously administered 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%). GLYX 13 is characterized by its rapid-acting and long-lasting antidepressant effects, as well as its robust cognitive enhancement capabilities due to its ability to both inhibit and enhance NMDA receptor-mediated signal transduction.
Uses
Used in Pharmaceutical Industry:
GLYX 13 is used as an antidepressant for the treatment of depressive disorders, specifically targeting treatment-resistant major depressive disorder. It is effective in providing rapid-acting and long-lasting relief from depressive symptoms, making it a promising candidate for patients suffering from severe and persistent depression.
GLYX 13 is also used as a cognitive enhancer, due to its ability to modulate NMDA receptor-mediated signal transduction. This property makes it a potential therapeutic agent for conditions involving cognitive impairment or decline.
Used in Neurological Applications:
GLYX 13 is used as an activator of the NMDA (N-methyl-D-aspartate) receptor, which plays a crucial role in learning, memory, and synaptic plasticity. By modulating the activity of this receptor, GLYX 13 has the potential to improve cognitive function and treat various neurological conditions associated with cognitive decline or impairment.
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.