Month: November 2022

On May 12, 2011, Conn, P. Jeffrey; Lindsley, Craig W.; Hopkins, Corey R.; Weaver, Charles David; Niswender, Colleen M.; Cheung, Yiu-Yin published a patent.Formula: C7H7FS The title of the patent was Aryl and heteroaryl sulfones as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction. And the patent contained the following:

The present invention relates to (hetero)aryl sulfone compounds which are useful as allosteric potentiators/pos. allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4), synthetic methods for making the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, for example, in treating neurol. and psychiatric disorders or other diseases associated with glutamate dysfunction. Preparation of 5-(2-chlorobenzylsulfonyl)-2-(pyridin-2-yl)-1H-benzo[d]imidazole was exemplified (yield 59%). The experimental process involved the reaction of (2-Fluorophenyl)methanethiol(cas: 72364-46-6).Formula: C7H7FS

The Article related to aryl sulfone preparation mglur4 receptor potentiator neurol psychiatric disease, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Formula: C7H7FS

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On April 30, 2011, Dey, Raja; Chen, Lin published an article.Computed Properties of 32462-30-9 The title of the article was In search of allosteric modulators of α7-nAChR by solvent density guided virtual screening. And the article contained the following:

Nicotinic acetylcholine receptors (nAChR) are pentameric ligand gated ion channels whose activity can be modulated by endogenous neurotransmitters as well as by synthetic ligands that bind the same or distinct sites from the natural ligand. The subtype of α7 nAChR has been considered as a potential therapeutic target for Alzheimer’s disease, schizophrenia, and other neurol. and psychiatric disorders. A homol. model was developed for α7 nAChR based on 2 high resolution crystal structures with Brookhaven Protein Data Bank (PDB) codes 2QC1 and 2WN9 for threading on one monomer and then for building a pentamer, resp. A number of small mol. binding sites are identified using Pocket Finder of Internal Coordinate Mechanics (ICM). Remarkably, these computer-identified sites match perfectly with ordered solvent densities found in the high-resolution crystal structure of α1 nAChR, suggesting that the surface cavities in the α7 nAChR model are likely binding sites of small mols. A high throughput virtual screening by flexible ligand docking of 5008 small mol. compounds was performed at 3 potential allosteric modulator (AM) binding sites of α7 nAChR using Molsoft ICM software. Some exptl. verified allosteric modulators of α7 (CCMI comp-6, LY 7082101, 5-HI, TQS, PNU-120596, genistein, and NS-1738) ranked among top 100 compounds, while the rest of the compounds in the list could guide further search for new allosteric modulators. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Computed Properties of 32462-30-9

The Article related to nicotinic acetylcholine receptor allosteric modulator virtual screening homol modeling, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Computed Properties of 32462-30-9

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On March 25, 2010, Gant, Thomas G.; Shahbaz, Manouchehr M. published a patent.Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol The title of the patent was Preparation of deuterated carisoprodol as carbamate reducers of skeletal muscle tension with improved pharmacokinetics, pharmacodynamics, and toxicity properties. And the patent contained the following:

The present invention relates to novel carisoprodol of formula (I) (wherein R1-R24 are each independently selected from the group consisting of hydrogen and deuterium; and at least one of R1-R24 is deuterium) to be used as new carbamate skeletal muscle relaxants, pharmaceutical compositions thereof, and methods of use thereof. The carisoprodol compounds may be used for the treatment of a skeletal muscle tension-mediated disorder, such as musculoskeletal pain and hypertonia. The experimental process involved the reaction of 2-Methyl-2-propylpropane-1,3-diol(cas: 78-26-2).Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol

The Article related to carisoprodol deuterium derivative preparation skeletal muscle relaxant stability toxicity, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Recommanded Product: 2-Methyl-2-propylpropane-1,3-diol

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On August 5, 2004, Groppi, Vincent Edward, Jr.; Rogers, Bruce Nelsen; Rudmann, Daniel Gregory published a patent.Name: (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol The title of the patent was Treatment of diseases with alpha-7 NACh receptor full agonists. And the patent contained the following:

The present invention relates to compositions and methods to treat diseases or conditions with alpha-7 nicotinic acetylcholine receptor (AChR) full agonists by decreasing levels of tumor necrosis factor-alpha and/or by stimulating vascular angiogenesis. The experimental process involved the reaction of (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol(cas: 280752-78-5).Name: (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol

The Article related to nicotinic acetylcholine receptor agonist quinuclidinylheteroarylamide cancer diabetes angiogenesis therapy, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Name: (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol

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On November 30, 2017, Foster, Alan C.; Rangel-Diaz, Natalie; Staubli, Ursula; Yang, Jia-Ying; Penjwini, Mahmud; Viswanath, Veena; Li, Yong-Xin published an article.Name: H-Phg(4-OH)-OH The title of the article was Phenylglycine analogs are inhibitors of the neutral amino acid transporters ASCT1 and ASCT2 and enhance NMDA receptor-mediated LTP in rat visual cortex slices. And the article contained the following:

The N-methyl-D-aspartate receptor (NMDA) co-agonist D-serine is a substrate for the neutral amino acid transporters ASCT1 (SLC1A4) and ASCT2 (SLC1A5). We identified L-phenylglycine (PG) and its analogs as inhibitors of ASCT1 and ASCT2. PG analogs were shown to be non-substrate inhibitors of ASCT1 and ASCT2 with a range of activities relative to other amino acid transport systems, including sodium-dependent glutamate transporters, the sodium-independent D-serine transporter asc-1 and system L. L-4-chloroPG was the most potent and selective ASCT1/2 inhibitor identified. The PG analogs facilitated theta-burst induced long-term potentiation in rat visual cortex slices in a manner that was dependent on extracellular D-serine. For structurally-related PG analogs, there was an excellent correlation between ASCT1/2 transport inhibition and enhancement of LTP which was not the case for inhibition of asc-1 or system L. The ability of PG analogs to enhance LTP is likely due to inhibition of D-serine transport by ASCT1/2, leading to elevated extracellular levels of D-serine and increased NMDA receptor activity. These results suggest that ASCT1/2 may play an important role in regulating extracellular D-serine and NMDA receptor-mediated physiol. effects and that ASCT1/2 inhibitors have the potential for therapeutic benefit. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Name: H-Phg(4-OH)-OH

The Article related to l phenylglycine asct1 asct2 inhibitor long term potentiation, asct1, asct2, d-serine, ltp, nmda, phenylglycine, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Name: H-Phg(4-OH)-OH

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On September 29, 2017, Shen, Peng; Hu, Qingchuan; Dong, Meixue; Bai, Shunjie; Liang, Zihong; Chen, Zhi; Li, Pengfei; Hu, Zicheng; Zhong, Xiaogang; Zhu, Dan; Wang, Haiyang; Xie, Peng published an article.Reference of H-Phg(4-OH)-OH The title of the article was Venlafaxine exerts antidepressant effects possibly by activating MAPK-ERK1/2 and P13K-AKT pathways in the hippocampus. And the article contained the following:

Serotonin noradrenaline reuptake inhibitors are effective antidepressant drugs, which include venlafaxine and duloxetine. Venlafaxine is commonly used in a clin. context, but the mol. biol. mechanisms behind its effects have not been fully determined Here, we explored the potential biol. effects of venlafaxine on mouse hippocampus. Mice were randomly divided into two groups and injected daily with 0.9% NaCl solution or venlafaxine. A GC-MS-based metabolomic approach was used to identify possible metabolic differences between these groups, and the key proteins involved in the relevant pathways were validated by western blotting. In our experiments, 27 hippocampal metabolites that distinguished the venlafaxine group from the control group were identified. These differential metabolites were subjected to Ingenuity Pathway Anal., which revealed that they were strongly related to two metabolic pathways (MAPK-ERK1/2 and P13K-AKT signaling pathways). Six key proteins, BDNF, p-c-Raf, p-MAPK, p-MEK, p-AKT, and CREB, were verified by western blotting and the results were consistent with the differential metabolites identified by GC-MS. This study sheds light on the biol. mechanisms underlying the effects of venlafaxine. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Reference of H-Phg(4-OH)-OH

The Article related to venlafaxine antidepressant hippocampus mapk erk1 erk2 p13k akt, antidepressant, hippocampus, mechanism, metabolomics, venlafaxine, western blotting, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Reference of H-Phg(4-OH)-OH

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Grabska-Kobylecka, Izabela; Kaczmarek-Bak, Justyna; Figlus, Malgorzata; Prymont-Przyminska, Anna; Zwolinska, Anna; Sarniak, Agata; Wlodarczyk, Anna; Glabinski, Andrzej; Nowak, Dariusz published an article in 2020, the title of the article was The presence of caffeic acid in cerebrospinal fluid: evidence that dietary polyphenols can cross the blood-brain barrier in humans.Synthetic Route of 621-37-4 And the article contains the following content:

Epidemiol. data indicate that a diet rich in plant polyphenols has a pos. effect on brain functions, improving memory and cognition in humans. Direct activity of ingested phenolics on brain neurons may be one of plausible mechanisms explaining these data. This also suggests that some phenolics can cross the blood-brain barrier and be present in the brain or cerebrospinal fluid. We measured 12 phenolics (a combination of the solid-phase extraction technique with high-performance liquid chromatog.) in cerebrospinal fluid and matched plasma samples from 28 patients undergoing diagnostic lumbar puncture due to neurol. disorders. Homovanillic acid, 3-hydroxyphenyl acetic acid and caffeic acid were detectable in cerebrospinal fluid reaching concentrations (median; interquartile range) 0.18; 0.14μmol/L, 4.35; 7.36μmol/L and 0.02; 0.01μmol/L, resp. Plasma concentrations of caffeic acid (0.03; 0.01μmol/L) did not correlate with those in cerebrospinal fluid (ρ = -0.109, p = 0.58). Because food (fruits and vegetables) is the only source of caffeic acid in human body fluids, our results indicate that the same dietary phenolics can cross blood-brain barrier in humans, and that transportation of caffeic acid through this barrier is not the result of simple or facilitated diffusion. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Synthetic Route of 621-37-4

The Article related to caffeic acid dietary polyphenol blood brain barrier cerebrospinal fluid, blood-brain barrier, caffeic acid, cerebrospinal fluid, dietary polyphenols, plant phenolics, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Synthetic Route of 621-37-4

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On August 15, 2022, Seppala, Ari; Turunen, Konsta; Yazdani, Maryam Roza published an article.Electric Literature of 585-88-6 The title of the article was Thermal conductivity of sugar alcohols. And the article contained the following:

During the past decade sugar alcs. have been extensively studied for thermal storage purposes. One of the recent focuses of research has been in improving their heat charge and discharge rate by enhancing the thermal conductivity with different types of additives. However, the current literature shows a vast discrepancy in measured values of sugar alcs. This work presents an exptl. study on thermal conductivity of seven sugar alcs. The aim is to find out the reason for the discrepancy of literature values for erythritol, mannitol and xylitol, and to present new reference data for galacticol, myo-inositol, maltitol and sorbitol. We study the impact of material preparation method, raw material grade and sensor contact on the crystalline structure and the conductivity The crystalline structure was inspected with optical and SEM and X-ray diffraction, and melting properties with differential scanning calorimetry. We found that different polymorphs, grain structure and crystallite sizes can be obtained by different preparation methods. This caused the conductivity of mannitol, galacticol and myo-inositol to vary by tens of percentages. Crystallization temperatures of xylitol and erythritol were found to affect their grain size but had only a minor effect on the conductivity Overall, the conductivities of solid phase sugar alcs. were found to be within the upper range of the previous literature; based on the methods of this work, we did not find any evidence for the low and intermediate values for erythritol, xylitol and mannitol. Due to the high amorphous content of maltitol and sorbitol their conductivity was substantially lower than that of the other sugar alcs. Thermal conductivity of liquid phases was found to accurately follow a linear relationship with the molar mass for sugar alcs. with carbon number between 4 and 6. The experimental process involved the reaction of SweetPearlR P300 DC Maltitol(cas: 585-88-6).Electric Literature of 585-88-6

The Article related to sugar alc thermal conductivity crystallization, Electrochemical, Radiational, and Thermal Energy Technology: Safety Aspects Of Energy Utilization and other aspects.Electric Literature of 585-88-6

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Madsen, H. T.; Soegaard, E. G. published an article in 2014, the title of the article was Fouling Formation During Hydrogen Sulfide Scavenging With 1,3,5-tri-(hydroxyethyl)-hexahydro-s-triazine.Electric Literature of 4719-04-4 And the article contains the following content:

To investigate if the hydrogen sulfide scavenger, 1,3,5-tri-(hydroxyethyl)-hexahydro-s-triazine, could explain a severe carbon/sulfur rich fouling found at a refinery, experiments were conducted to study the scavenging process and the composition of the fouling. The reaction was analyzed with electro spray ionization mass spectrometry (ESI-MS), and the fouling with IR spectroscopy and X-ray diffraction. The fouling was found to be a byproduct of the scavenging reaction, and to consist of dithiazine mols. with linking carbon-sulfur chains. ESI-MS anal. strongly indicates that these chains are generated when dithiazine decomposes to smaller mols., which through condensation reactions with dithiazine forms the fouling. The experimental process involved the reaction of 2,2′,2”-(1,3,5-Triazinane-1,3,5-triyl)triethanol(cas: 4719-04-4).Electric Literature of 4719-04-4

The Article related to triazine hydrogen sulfide scavenging fouling formation mechanism, Fossil Fuels, Derivatives, and Related Products: General Engineering Studies (Coal and Petroleum) and other aspects.Electric Literature of 4719-04-4

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On October 15, 1981, Jacobi, Haireddin; Opitz, Wolfgang published a patent.Synthetic Route of 72364-46-6 The title of the patent was S-Alkyl 3-(alkylthio)thiopropionates and their use in drugs. And the patent contained the following:

R1SCH2CH2C(O)SR [R, R1 = alkyl optionally substituted with amino, aryl, heteroaryl, etc., (in turn optionally substituted with 1-3 halo, alkyl, nitro, alkoxy, etc.), cycloalkyl] were prepared as inflammation inhibitors (no data). Thus 0.81 mL CH2:CHCOCl was added in portions to 4.28 g 3,4,5-(MeO)3C6H2CH2SH and 8 mL 5% NaOH at room temperature, and the mixture was stirred to the end of the exotherm to give 32.1% I. The experimental process involved the reaction of (2-Fluorophenyl)methanethiol(cas: 72364-46-6).Synthetic Route of 72364-46-6

The Article related to thio ester aralkyl antiinflammatory, propionate thio benzyl antiinflammatory, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Esters, Acyl Peroxides, Acyl Halides and other aspects.Synthetic Route of 72364-46-6

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