Maklad, Noha’s team published research in Chemtracts in 21 | CAS: 226878-01-9

Chemtracts published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C19H21N3O, Name: N-(Adamantan-1-yl)quinoxaline-2-carboxamide.

Maklad, Noha published the artcilePositive and negative modulation of group 1 metabotropic glutamate receptors, Name: N-(Adamantan-1-yl)quinoxaline-2-carboxamide, the publication is Chemtracts (2008), 21(5), 165-171, database is CAplus.

A review. Vanejevs et al. developed a pharmacophore hypothesis using potent and com. available metabotropic glutamate receptor 1 (mGluR1) analogs. This was done by aligning the potent and com. available mGluR1 antagonists using the flexible alignment tool included in the Mol. Operating Environment software. The developed pharmacophore model offers a new and different methodol. to discover such analogs.

Chemtracts published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C19H21N3O, Name: N-(Adamantan-1-yl)quinoxaline-2-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Ericson, Jon F.’s team published research in Environmental Science & Technology in 44 | CAS: 375815-87-5

Environmental Science & Technology published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Name: 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate.

Ericson, Jon F. published the artcileEvaluation of the OECD 314B Activated Sludge Die-Away Test for Assessing the Biodegradation of Pharmaceuticals, Name: 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, the publication is Environmental Science & Technology (2010), 44(1), 375-381, database is CAplus and MEDLINE.

The European Medicines Agency guideline for the environmental risk assessment of medicinal products provides a step-by-step phased approach to evaluate the potential risks of new medicines to the environment. Phase I (prescreen) estimates the initial exposure of the new medicine in the environment. Phase II A (screen) estimates the fate and effects in the environment. The fate screen determines the inherent properties of the new medicinal active ingredient to sorb to sludge, soil, and sediment matrixes and its potential to degrade in a sewage treatment plant and in the subsequent water-sediment compartment. Current ERA Guidance (2006) recommends the OECD 301B Ready Biodegradation Test for Phase II Tier A testing without a clear recommendation for Phase II Tier B testing when further refinement may be needed. With the recent approval of the OECD 314B method for activated sludge, there is now an alternative test method that may be better suited for Phase II Tier A testing and to the data needs of the ERA. As a batch test, it fits the needs of a Tier A screen. It is not designed to simulate the operational steps of a sewage treatment plant, such as the OECD 303 tests, and yet provides the following without considerable costs or resources of OECD 303: (1) useful kinetic information in a test that reflects the conditions of the sewage-treatment environment, i.e., realistic biomass solids concentrations and low level test material concentrations to simulate 1st-order (nongrowth) kinetics, (2) mass balance anal. for CO2 evolution and for residues found in mixed liquor, (3) use of an abiotic control to assess losses other than those attributed to biotic biodegradation, and (4) biotransformation profile of degradants. This paper presents the results of OECD 301B with that of OECD 314B for activated sludge biodegradation for 5 Pfizer drug substances. The use of this new method as an alternative to OECD 301B would strengthen the fate testing screen in Phase II Tier A of the EMEA ERA. It would provide a characterization of a substance’s potential for biotransformation and mineralization during sewage treatment and provide a means for revising predicted environmental concentration of surface water for amount removed during sewage treatment.

Environmental Science & Technology published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Name: 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Anonymous’s team published research in IP.com Journal in 9 | CAS: 375815-87-5

IP.com Journal published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Computed Properties of 375815-87-5.

Anonymous published the artcileA condensation product between 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2(11),3,5,7,9-pentaene and lactose, Computed Properties of 375815-87-5, the publication is IP.com Journal (2009), 9(3B2), 2, database is CAplus.

A reaction of L-tartaric acid with 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine (Chantix, varenicline) provided Chantix L-tartrate. A reaction of that compound with lactose [i.e., 4-O-β-D-galactopyranosyl-D-glucose] gave a mixture of 4-O-[6-(7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepin-8-yl)-β-D-galactopyranosyl]-β-D-glucopyranose and 4-O-(β-D-galactopyranosyl)-6-deoxy-6-(7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepin-8-yl)-β-D-glucopyranose.

IP.com Journal published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Computed Properties of 375815-87-5.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Zhang, Tao’s team published research in AAPS Journal in 23 | CAS: 375815-87-5

AAPS Journal published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C9H17NO, Recommanded Product: 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate.

Zhang, Tao published the artcileAssessing Food Effects on Oral Drug Absorption Based on the Degree of Renal Excretion, Recommanded Product: 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, the publication is AAPS Journal (2021), 23(3), 47, database is CAplus and MEDLINE.

Food intake influences the pharmacokinetics of orally administered drugs by altering drug absorption, metabolism, and excretion. A drug which is mainly excreted into urine as parent drug is usually highly water-soluble and metabolically stable. Food intake is not expected to significantly affect its extent of oral absorption, metabolism, and excretion. Therefore, we hypothesize that an orally administered drug with significant renal excretion should not have a dramatic food effect (FE). To test our hypothesis, we summarized the FE for orally administered immediate-release (IR) and modified-release (MR) formulations approved by the US FDA from 1998 to 2019, focusing on drugs undergoing significant renal excretion. Totally, 98 active pharmaceutical ingredients (APIs) in IR formulations and 34 APIs in MR formulations were selected. The results demonstrate that the area-under-the-curve (AUC) for IR drug products with fur_cunchanged_cpo > 10% is unlikely to be affected by food, although the peak plasma concentration (Cmax) may increase or decrease by up to 50%. Compared with IR drug products with fur_cunchanged_cpo > 10%, MR drug products with fur_cunchanged_cpo > 10% tend to have more significant FE. Although our proposed approach cannot substitute a clin. FE study, it could be a useful addition to early drug development to get an initial sense of the potential for FE for a drug candidate.

AAPS Journal published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C9H17NO, Recommanded Product: 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Colgan, Stephen T.’s team published research in Journal of Pharmaceutical Sciences in 105 | CAS: 375815-87-5

Journal of Pharmaceutical Sciences published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Category: quinoxaline.

Colgan, Stephen T. published the artcileUse of Activated Carbon in Packaging to Attenuate Formaldehyde-Induced and Formic Acid-Induced Degradation and Reduce Gelatin Cross-Linking in Solid Dosage Forms, Category: quinoxaline, the publication is Journal of Pharmaceutical Sciences (2016), 105(7), 2027-2031, database is CAplus and MEDLINE.

Formaldehyde and formic acid are reactive impurities found in commonly used excipients and can be responsible for limiting drug product shelf-life. Described here is the use of activated carbon in drug product packaging to attenuate formaldehyde-induced and formic acid-induced drug degradation in tablets and crosslinking in hard gelatin capsules. Several pharmaceutical products with known or potential vulnerabilities to formaldehyde-induced or formic acid-induced degradation or gelatin crosslinking were subjected to accelerated stability challenges in the presence and absence of activated carbon. The effects of time and storage conditions were determined For all of the products studied, activated carbon attenuated drug degradation or gelatin crosslinking. This novel use of activated carbon in pharmaceutical packaging may be useful for enhancing the chem. stability of drug products or the dissolution stability of gelatin-containing dosage forms and may allow for the (1) extension of a drug product’s shelf-life when the limiting attribute is a degradation product induced by a reactive impurity, (2) marketing of a drug product in hotter and more humid climatic zones than currently supported without the use of activated carbon, and (3) enhanced dissolution stability of products that are vulnerable to gelatin crosslinking.

Journal of Pharmaceutical Sciences published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Category: quinoxaline.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Zhang, Wei-hua’s team published research in Harbin Yike Daxue Xuebao in 46 | CAS: 226878-01-9

Harbin Yike Daxue Xuebao published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C25H23NO4, Formula: C19H21N3O.

Zhang, Wei-hua published the artcileCalcium sensing receptor is involved in neonate rat cardiomyocyte apoptosis induced by hypoxia/reoxygenation via regulating calcium concentration in mitochondria, Formula: C19H21N3O, the publication is Harbin Yike Daxue Xuebao (2012), 46(6), 534-538, database is CAplus.

Calcium sensing receptor (CaR) activation plays a role in the regulation of SR-mitochondrial inter-organelle Ca2+ signaling, causing apoptosis during ischemia/reperfusion (I/R). Neonatal rat cardiomyocytes were subjected to 3 h of hypoxia, followed by 6 h of reoxygenation. Ca2+ m were determined using x-rhod-1 and the mitochondrial membrane potential was detected with JC-1 during reoxygenation. The apoptotic rates detected by Hoechst33342 were lower in NPS-2390 + Ca + Ni + Cd + H-Re (±4)%, 2-APB + Ca + Ni + Cd + H-Re (18±4)% and Ru + Ca + Ni + Cd + H-Re (23±5)% groups than H-Re (33±6)%, Ca+Ni+Cd+H-Re (31±5)% and Gd+Ni+Cd+HRe (34±3)% groups. [Ca 2+] m was increased in the Ca + Ni + Cd + H-Re group. The mitochondria transmembrane potential was lower in Ca + Ni + Cd + H-Re group than that in 2-APB + Ca + Ni + Cd + H-Re and Ru + Ca + Ni + Cd + H-Re groups. CaR activation causes Ca2+ release from the SR into the mitochondria through IP3 Rs and induces cardiomyocyte apoptosis during hypoxia/reoxygenation.

Harbin Yike Daxue Xuebao published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C25H23NO4, Formula: C19H21N3O.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Xun, Caifang’s team published research in Spectroscopy Letters in 49 | CAS: 375815-87-5

Spectroscopy Letters published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C11H12O4, Related Products of quinoxaline.

Xun, Caifang published the artcileInteraction between varenicline tartrate and bovine serum albumin, Related Products of quinoxaline, the publication is Spectroscopy Letters (2016), 49(4), 304-310, database is CAplus.

This paper mainly investigated the interaction between varenicline tartrate and bovine serum albumin. The Stern-Volmer quenching constant and bimol. quenching rate constant were determined; furthermore, the fluorescence quenching mechanism between varenicline tartrate and bovine serum albumin was clarified. The binding constants and the number of binding sites were deduced from the double logarithm regression curve. Thermodn. parameters were calculated, which indicated that the binding process was spontaneous and the acting force were mainly hydrophobic forces. The binding distance was calculated to be 4.80 nm, which means that there was nonradiative energy transfer from varenicline tartrate to bovine serum albumin during the process. And the bovine serum albumin conformation affected by varenicline tartrate was analyzed through UV-visible and synchronous fluorescence spectroscopy.

Spectroscopy Letters published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C11H12O4, Related Products of quinoxaline.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Sun, Ji-Fu’s team published research in Neuroscience Letters in 646 | CAS: 226878-01-9

Neuroscience Letters published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C6H5F4NO3S, Recommanded Product: N-(Adamantan-1-yl)quinoxaline-2-carboxamide.

Sun, Ji-Fu published the artcileCaSR and calpain contribute to the ischemia reperfusion injury of spinal cord, Recommanded Product: N-(Adamantan-1-yl)quinoxaline-2-carboxamide, the publication is Neuroscience Letters (2017), 49-55, database is CAplus and MEDLINE.

Spinal cord ischemia reperfusion injury (SCIRI) can cause spinal cord dysfunction and even devastating paraplegia. Calcium-sensing receptor (CaSR) and calpain are two calcium related mols. which have been reported to be involved in the ischemia reperfusion injury of cardiomyocytes and the subsequent apoptosis. Here, we studied the expression of CaSR and calpain in spinal cord neurons and tissues, followed by the further investigation of the role of CaSR/calpain axis in the cellular apoptosis process during SCIRI. The results of in vitro and in vivo studies showed that the expression of CaSR and calpain in spinal cord neurons increased during SCIRI. Moreover, the CaSR agonist GdCl3 and antagonist NPS-2390 enhanced or decreased the expression of CaSR and calpain resp. The expressions of CaSR and calpain were also consistent with the cellular apoptosis in spinal cord. Taken together, CaSR-calpain contributes to the SCIRI apoptosis, and CaSR antagonist might be a helpful drug for alleviating SCIRI.

Neuroscience Letters published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C6H5F4NO3S, Recommanded Product: N-(Adamantan-1-yl)quinoxaline-2-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Pei, Gaofeng’s team published research in Fundamental Research in 2 | CAS: 375815-87-5

Fundamental Research published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Category: quinoxaline.

Pei, Gaofeng published the artcileCEBIT screening for inhibitors of the interaction between SARS-CoV-2 spike and ACE2, Category: quinoxaline, the publication is Fundamental Research (2022), 2(4), 562-569, database is CAplus.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection, causing COVID-19, is the most challenging pandemic of the modern era. It has resulted in over 5 million deaths worldwide. To quickly explore therapeutics for COVID-19, we utilized a previously-established system, namely CEBIT. We performed a high-throughput screening of FDA-approved drugs to inhibit the interaction between the receptor-binding domain (RBD) of SARS-CoV-2 spike protein and its obligate receptor ACE2. This interaction is essential for viral entry and therefore represents a promising therapeutic target. Based on the recruitment of interacting mols. into phase-separated condensates as a readout, we identified six pos. candidates from a library of 2572 compounds, most of which have been reported to inhibit the entry of SARS-CoV-2 into host cells. Our surface plasmon resonance (SPR) and mol. docking analyses revealed the possible mechanisms via which these compounds interfere with the interaction between RBD and ACE2. Hence, our results indicate that CEBIT is highly versatile for identifying drugs against SARS-CoV-2 entry, and targeting CoV-2 entry by small mol. drugs is a viable therapeutic option to treat COVID-19 in addition to commonly used monoclonal antibodies.

Fundamental Research published new progress about 375815-87-5. 375815-87-5 belongs to quinoxaline, auxiliary class Neuronal Signaling,AChR,Natural product, name is 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate, and the molecular formula is C17H19N3O6, Category: quinoxaline.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider

 

Zhu, Yiran’s team published research in Ecotoxicology and Environmental Safety in 179 | CAS: 226878-01-9

Ecotoxicology and Environmental Safety published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C10H12O5, Product Details of C19H21N3O.

Zhu, Yiran published the artcileEffects of Cr(VI)-induced calcium-sensing receptor activation on DF-1 cell pyroptosis, Product Details of C19H21N3O, the publication is Ecotoxicology and Environmental Safety (2019), 257-264, database is CAplus and MEDLINE.

This study aims to investigate the effects of Cr(VI)-induced calcium-sensing receptor (CaSR) activation on DF-1 cell pyroptosis. Previous studies show that Cr(VI) could accumulate in the body of chickens and change Ca levels. Hence, a Ca-related pathway may be an important mechanism participating in some pathol. processes. Pyroptosis level, which is meditated by CaSR, increases under Cr(VI) accumulation. In the present study, pyroptosis was determined by flow cytometry to detect SYTOX blue and caspase-1 staining followed by morphol. observation. Interleukin (IL)-1β and IL-18 levels were detected by ELISA, while CaSR protein and [Ca2+]i contents were detected by Western blot and fluorescence microplate spectrophotometry, resp. The results showed that Cr(VI) causes DF-1 cell pyroptosis in a time- and dose-dependent manner and that this effect is caspase-1 dependent. Further experiments indicated that pyroptosis could be induced by Cr(VI) and is accompanied by up-regulated [Ca2+]i content. CaSR inhibition led to decreases in pyroptosis level. Some mechanisms may be involved in Cr(VI)-triggered CaSR activation and enhance DF-1 cell pyroptosis. Taken together, the results of this study support future investigations on Cr(VI)-induced pyroptosis in DF-1 cells.

Ecotoxicology and Environmental Safety published new progress about 226878-01-9. 226878-01-9 belongs to quinoxaline, auxiliary class Neuronal Signaling,mGluR, name is N-(Adamantan-1-yl)quinoxaline-2-carboxamide, and the molecular formula is C10H12O5, Product Details of C19H21N3O.

Referemce:
https://en.wikipedia.org/wiki/Quinoxaline,
Quinoxaline | C8H6N2 | ChemSpider