Category: 154235-83-3

AMPAkines Have Novel Analgesic Properties in Rat Models of Persistent Neuropathic and Inflammatory Pain was written by Le, Alexander M.;Lee, Michelle;Su, Chen;Zou, Anthony;Wang, Jing. And the article was included in Anesthesiology in 2014.Synthetic Route of C14H15N3O This article mentions the following:

Background: Novel analgesics that do not suppress the respiratory drive are urgently needed. Glutamate signaling through α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors plays important roles in central pain circuits. AMPAkines augment AMPA receptor function and have been shown to stimulate the respiratory drive to oppose opioid-induced hypoventilation. However, their role in chronic pain states remains unknown. Methods: The authors studied AMPAkines (CX546 and CX516) in rat spared nerve injury (SNI) model of neuropathic pain and Complete Freund’s Adjuvant (CFA) model of inflammatory pain. They measured the effect of AMPAkines on mech. and cold allodynia. They also evaluated their effect on depressive symptoms of pain using the forced swim test, as time of immobility on this test has been used as a measure for behavioral despair, a feature of depression. Results: The authors found that CX546, compared with DMSO (DMSO) control, reduced both mech. and sensory allodynia in SNI (DMSO group, n = 9; CX546 group, n = 11) and CFA models (both DMSO and CX546 groups, n = 9). They found that CX546, compared with control, also reduced depressive symptoms of pain by decreasing immobility on the forced swim test in both SNI (both DMSO and CX546 groups, n = 8) and CFA models (both DMSO and CX546 groups, n = 10). Finally, they found that CX516, compared with control, also reduced mech. and cold allodynia in the SNI model (both DMSO and CX516 groups, n = 10). Conclusions: AMPAkines alleviate pain hypersensitivity as well as depression-like behavior associated with long-lasting nerve injury and inflammatory insult. In the experiment, the researchers used many compounds, for example, Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3Synthetic Route of C14H15N3O).

Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3) belongs to quinoxaline derivatives. Quinoxalines have received a significant amount of attention due to their potential use in fighting various pathophysiological conditions like epilepsy, Parkinson’s, and Alzheimer’s diseases. They are well-known for application in organic light emitting devices, polymers and pharmaceutical agents. The quinoxaline-containing polymers are applicable in optical devices due to their thermal stability and low band gap.Synthetic Route of C14H15N3O

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Meta-analysis of the efficacy of adjunctive NMDA receptor modulators in chronic schizophrenia was written by Singh, Surendra P.;Singh, Vidhi. And the article was included in CNS Drugs in 2011.COA of Formula: C14H15N3O This article mentions the following:

Background: Based on the glutamatergic NMDA receptor hypofunction theory of schizophrenia, NMDA receptor modulators (NMDARMs) may have therapeutic potential in the treatment of schizophrenia. Objective: This meta-anal. aimed to evaluate the potential of modulators of the NMDA receptor as adjunctive therapy for schizophrenia, using the results from published trials. Data Sources: A primary electronic search for controlled clin. trials using NMDARMs in schizophrenia was conducted on the PubMed, Cochrane Library, EMBASE, CINAHL and PsycINFO databases. A secondary manual search of references from primary publications was also performed. Study Selection: Inclusion criteria were the application of an established method of diagnosis, randomized case assignment, comparison of NMDARM add-on therapy with placebo, and double-blind assessment of symptoms in chronic schizophrenia using standardized rating scales. Results were based on a total sample size of 1253 cases from 29 trials that fulfilled the specified criteria. Data Extraction: Scores on rating scales or on their relevant subscales were obtained for all selected studies from published results for the min. dataset to compute the difference between post- and pre-trial scores and their pooled standard deviation for NMDARM add-on therapy and placebo groups for neg., pos. and total symptoms. Results: A neg. standardized mean difference (SMD) indicates therapeutic benefit in favor of NMDARM add-on therapy and all SMD results mentioned here are statistically significant. The overall effect size for NMDARMs as a group was small for neg. (SMD -0.27) and medium for total (SMD -0.40) symptoms of chronic schizophrenia. Subgroup anal. revealed medium effect sizes for D-serine and N-acetyl-cysteine (NAC) for neg. (SMD -0.53 and -0.45, resp.) and total (SMD -0.40 and -0.64, resp.) symptoms, and for glycine (SMD -0.66) and sarcosine (SMD -0.41) for total symptoms. As adjuvants to non-clozapine antipsychotics, addnl. therapeutic benefits were observed for NMDARM as a group (SMD -0.14) and glycine (SMD -0.54) for pos. symptoms; D-serine (SMD -0.54), NAC (SMD -0.45) and sarcosine (SMD -0.39) for neg. symptoms; and NMDARM as a group (SMD -0.38), D-serine (SMD -0.40), glycine (SMD -1.12), NAC (SMD -0.64) and sarcosine (SMD -0.53) for total symptoms. When added to clozapine, none of the drugs demonstrated therapeutic potential, while addition of glycine (SMD +0.56) worsened pos. symptoms. Conclusions: Taking into consideration the number of trials and sample size in subgroup analyses, D-serine, NAC and sarcosine as adjuncts to non-clozapine antipsychotics have therapeutic benefit in the treatment of neg. and total symptoms of chronic schizophrenia. While glycine improves pos. and total symptoms as an adjuvant to non-clozapine antipsychotics, it worsens them when added to clozapine. In the experiment, the researchers used many compounds, for example, Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3COA of Formula: C14H15N3O).

Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3) belongs to quinoxaline derivatives. Compounds possessing quinoxaline derivatives were bestowed with a variety of significant biological properties such as antiviral, antimalarial, anticancer, DNA intercalation, DNA duplex stabilization, and many others. Modifying quinoxaline structure it is possible to obtain a wide variety of biomedical applications, namely antimicrobial activities and chronic and metabolic diseases treatment.COA of Formula: C14H15N3O

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

CX-516 Cortex Pharmaceuticals Inc was written by Danysz, W.. And the article was included in Current Opinion in Central & Peripheral Nervous System Investigational Drugs in 1999.Safety of Piperidin-1-yl(quinoxalin-6-yl)methanone This article mentions the following:

A review with many references CX-516, an AMPA modulator from Cortex Pharmaceuticals, is in phase I/IIa clin. trials for the symptomatic treatment of deficits in memory and cognition in Alzheimer’s disease (AD) and similar disorders. CX-516 and other members in the series are also being investigated for possible antidepressant and antipsychotic activity. Results from initial studies showed that CX-691 and CX-519, both members of the AMP Akine family, have antidepressant activities. In Jan. 1999, Cortex licensed AMP Akine technol. rights to Organon for schizophrenia and depression. Cortex entered into a Cooperative Research and Development Agreement (CRADA) with the National Institute of Neurol. Diseases and Stroke, National Institutes of Health, for the initial clin. evaluation of CX-516 in AD patients in Nov. 1996. The results of a trial of CX-516 in combination with clozapine in schizophrenia patients were presented at the International Society for Schizophrenia Research in Apr. 1999. CX-516 improved a number of aspects of cognitive function. In the experiment, the researchers used many compounds, for example, Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3Safety of Piperidin-1-yl(quinoxalin-6-yl)methanone).

Piperidin-1-yl(quinoxalin-6-yl)methanone (cas: 154235-83-3) belongs to quinoxaline derivatives. Condensed heterocycles of quinoxalines have become attractive targets in synthetic and medicinal chemistry due to their significant biological activities. Quinoxalines are used in the treatment of bacterial, cancer, and HIV infections. Moreover, varenicline, a clinical drug is used for treating nicotine addiction, also contains quinoxaline moiety.Safety of Piperidin-1-yl(quinoxalin-6-yl)methanone

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider