Month: January 2021

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Aceclidine effects on outflow facility after ciliary muscle disinsertion

Aceclidine increases outflow facility with little accomodative effect. To determine whether this dissociation resides in the ciliary muscle (CM) or trabecular meshwork (TM), we measured aceclidine effects on perfusion outflow facility in both eyes of 8 rhesus monkeys after unilateral disinsertion of the CM from the TM. Facility in the control eyes increased by ~250% following intravenous pilocarpine and by an additional ~250% following intravenous pilocarpine and by an additional ~250% following intracameral pilocarpine, relative to baseline and uncorrected for washout. In CM-disinserted eyes, the facility response to intravenous and intracameral pilocarpine averaged ~25% of that in contralateral controls. Cytochalasin B, which acts directly on the TM to increase facility but is not additive to maximal pilocarpine doses in normal eyes, had no additional effect beyond that of pilocarpine in control eyes but induced an additional 100% facility increase relative to baseline in CM-disinserted eyes. The accomodative response to carbachol in CM-disinserted eyes was ~80% of that in contralateral controls, consistent with retention of CM contractility and the gonioscopic appearance of shallow CM disinsertion. Intracameral aceclidine HCl doses of 5 and 50 mug increased outflow facility by ~80 and 250%, respectively, in control eyes, and by ~0 and 80% in Cm-disinserted eyes. Either the low aceclidine dose affected facility via the CM, while the high dose exerted an additional effect on the TM, or aceclidine acted only via the CM, with the low dose being ineffective and the high dose modestly effective in CM-disinserted eyes because only a few CM-TM attachments remained.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H64N | ChemSpider

Synthetic Route of 827-61-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Article£¬once mentioned of 827-61-2

Metabolomics responses of Bambusa pervariabilis ¡Á Dendrocalamopsis grandis varieties to Biotic (pathogenic fungus) stress

Bambusa pervariabilis ¡Á Dendrocalamopsis grandis blight, caused by Arthrinium phaeospermum, is one of the most common and serious diseases in bamboo and occurs in the newly born twigs. Bamboo has suffered large dead areas, including more than 3000 hm2, which greatly threatens the process of returning farmlands to forests and the construction of ecological barriers. To identify differential metabolites and metabolic pathways associated with B. pervariabilis ¡Á D. grandis to A. phaeospermum, ultra-performance liquid chromatography (UPLC) and quadrupole-time of flight (Q-TOF) Mass Spectrometry (MS) combined with a data-dependent acquisition method was used to analyse the entire sample spectrum. In total, 13223 positive ion peaks and 10616 negative ion peaks were extracted. OPLS-DA and several other analyses were performed using the original data. The OPLS-DA models showed good quality and had strong predictive power, indicating clear trends in the analyses of the treatment and control groups. Clustering and KEGG pathway analyses were used to screen the differential metabolites in the treatment and control groups from the three B. pervariabilis ¡Á D. grandis varieties and reflected their metabolic responses induced by A. phaeospermum infection. The results showed that the three B. pervariabilis ¡Á D. grandis varieties mode showed significant changes in the following six resistance-related metabolites after A. phaeospermum invasion in positive and negative ion modes: proline, glutamine, dictamnine, apigenin 7-O-neohesperidoside, glutamate, and cis-Aconitate. The following four main metabolic pathways are involved: Arginine and proline metabolism, Glyoxylate and dicarboxylate metabolism, Biosynthesis of alkaloids derived from shikimate pathway, and Flavone and flavonol biosynthesis. This study lays a foundation for the later detection of differential metabolites and metabolic pathways for targeting, and provides a theoretical basis for disease-resistant breeding and the control of B. pervariabilis ¡Á D. grandis blight.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H68N | ChemSpider

Related Products of 827-61-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Article£¬once mentioned of 827-61-2

IDrugs and idevices discovery research: Preclinical assays, techniques, and animal model studies for ocular hypotensives and neuroprotectants

Discovery ophthalmic research is centered around delineating the molecular and cellular basis of ocular diseases and finding and exploiting molecular and genetic pathways associated with them. From such studies it is possible to determine suitable intervention points to address the disease process and hopefully to discover therapeutics to treat them. An investigational new drug (IND) filing for a new small-molecule drug, peptide, antibody, genetic treatment, or a device with global health authorities requires a number of preclinical studies to provide necessary safety and efficacy data. Specific regulatory elements needed for such IND-enabling studies are beyond the scope of this article. However, to enhance the overall data packages for such entities and permit high-quality foundation-building publications for medical affairs, additional research and development studies are always desirable. This review aims to provide examples of some target localization/verification, ocular drug discovery processes, and mechanistic and portfolio-enhancing exploratory investigations for candidate drugs and devices for the treatment of ocular hypertension and glaucomatous optic neuropathy (neurodegeneration of retinal ganglion cells and their axons). Examples of compound screening assays, use of various technologies and techniques, deployment of animal models, and data obtained from such studies are also presented.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about Related Products of 827-61-2

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Quinuclidine – Wikipedia,
Quinuclidine | C7H82N | ChemSpider

Electric Literature of 123536-14-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Patent£¬once mentioned of 123536-14-1

SUBSTITUTED SPIRO-AMIDE COMPOUNDS

Substituted spiro-amide compounds corresponding to formula 1 in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Electric Literature of 123536-14-1, you can also check out more blogs aboutElectric Literature of 123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H129N | ChemSpider

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 827-61-2, Name is Quinuclidin-3-yl acetate,introducing its new discovery., name: Quinuclidin-3-yl acetate

Visible-Light-Mediated Metal-Free Difunctionalization of Alkenes with CO2 and Silanes or C(sp3)?H Alkanes

Catalytic alkene difunctionalization via Si?H and C?H activations represents an ideal atom- and step-economic pathway for quick assembly of molecular complexity. We herein developed a visible-light-promoted metal-free difunctionalization of alkenes using abundant CO2 and readily available Si?H and C(sp3)?H bonds as feedstocks. Through the merger of photoredox and hydrogen-atom-transfer catalysis, a variety of value-added compounds, such as beta-silacarboxylic acids and acids bearing a gamma-heteroatom (e.g., N, O, S) could be directly accessed from simple alkenes in a redox-neutral fashion.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. name: Quinuclidin-3-yl acetate, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 827-61-2, in my other articles.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H63N | ChemSpider

Related Products of 827-61-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Article£¬once mentioned of 827-61-2

A practical chemoenzymatic process to access (R)-quinuclidin-3-ol on scale

(¡À)-3-Butyryloxyquinuclidinium butyrate 6 (2 M, 571 g/L), prepared from (¡À)-quinuclidin-3-ol 1 and butyric anhydride, undergoes enantioselective hydrolysis by an Aspergillus melleus protease {1.0% (w/v)} in water in the presence of Ca(OH)2 to keep the reaction at pH 7 and trap butyric acid that is introduced as part of (¡À)-6 and generated by the enzymatic hydrolysis. After a 24 h period, extraction with n-heptane provides (R)-quinuclidin-3-yl butyrate 5a, which, on methanolysis with Na2CO3, is converted into (R)-1, a common pharmacophore of neuromodulators acting on muscarinic receptors, in 96% ee and 42% overall yield from (¡À)-1. The unwanted antipode (S)-1, which is extracted into n-butanol and purified via its hydrochloride salt in 89% ee and 40% overall yield from (¡À)-1, can be racemized by the catalysis of Raney Co at 140C under an atmosphere of H2 (5 kg/cm2) to regenerate (¡À)-1 in 97% yield.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H75N | ChemSpider

Electric Literature of 5291-32-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.5291-32-7, Name is APR-246, molecular formula is C10H17NO3. In a Article£¬once mentioned of 5291-32-7

Mutant p53 tunes the NRF2-dependent antioxidant response to support survival of cancer cells

NRF2 (NFE2L2) is one of the main regulators of the antioxidant response of the cell. Here we show that in cancer cells NRF2 targets are selectively upregulated or repressed through a mutant p53-dependent mechanism. Mechanistically, mutant p53 interacts with NRF2, increases its nuclear presence and resides with NRF2 on selected ARE containing gene promoters activating the transcription of a specific set of genes while leading to the transcriptional repression of others. We show that thioredoxin (TXN) is a mutant p53-activated NRF2 target with pro-survival and pro-migratory functions in breast cancer cells under oxidative stress, while heme oxygenase 1 (HMOX1) is a mutant p53-repressed target displaying opposite effects. A gene signature of NRF2 targets activated by mutant p53 shows a significant association with bad overall prognosis and with mutant p53 status in breast cancer patients. Concomitant inhibition of thioredoxin system with Auranofin and of mutant p53 with APR-246 synergizes in killing cancer cells expressing p53 gain-of-function mutants.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H172N | ChemSpider

Related Products of 827-61-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Patent£¬once mentioned of 827-61-2

Optically active 3 – the preparation method of the quinine is mellow (by machine translation)

The invention relates to a method for synthesizing intermediate, which belongs to the field of organic synthesis. In particular to a simple operation, low cost, and is suitable for industrial production of optically active 3 – the preparation method of the quinine is mellow. In order to 4 – piperidine carboxylic acid as the starting material, through esterification, pro-nuclear substituted, Dieckmann condensation, decarboxylation, salt, reduction, acetylation, chemically so as to obtain the intermediate optically active 3 – the quinine is mellow. The above reaction equation is as follows: (by machine translation)

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Quinuclidine – Wikipedia,
Quinuclidine | C7H35N | ChemSpider

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Safety of Quinuclidin-3-yl acetate, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2

Design, Synthesis, and Neurochemical Evaluation of 5-(3-Alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 Muscarinic Receptor Agonists

A series of 5-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines (7a-h) was synthesized for biological evaluation as selective agonists for M1 receptors coupled to phosphoinositide (PI) metabolism in the central nervous system.Each ligand bound with high affinity to muscarinic receptors from rat brain as measured by inhibition of <3H>-(R)-quinuclidinyl benzilate (<3H>-(R)-QNB) binding. 5-(3-Methyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine trifluoroacetate (CDD-0098-J; 7a)displayed high affinity (IC50 = 2.7 +/- 0.69 muM) and efficacy at muscarinic receptors coupled to PI metabolism in the rat cortex and hippocampus .Increasing the length of the alkyl substituent increased affinity for muscarinic receptors yet decreased activity in PI turnover assays.The hippocampal PI response of 7a was blocked by lower concentrations of pirenzepine (8) or by higher concentrations of either AF-DX 116 (9) or p-fluorohexahydrosiladifenidol (10), suggesting that a low concentrations 7a selectively stimulates PI turnover through M1 receptors.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H53N | ChemSpider

Synthetic Route of 5291-32-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.5291-32-7, Name is APR-246, molecular formula is C10H17NO3. In a Patent£¬once mentioned of 5291-32-7

2-SULFONYLPYRIMIDINES

The invention relates to 2-sulfonylpyrimidine compounds and salts and solvates thereof for use in the treatment of a proliferative disease such as cancers. The 2- sulfonyl-primidine compounds may be administered, either simultaneously or sequentially, with one or more pharmacologically active compounds and salts and solvates thereof such as an inhibitor of glutamate cysteine ligase. The 2- sulfonylpyrimidine compound may be represented by formula (I): (I) wherein: R1 is selected from C1-6 alkyl, C6-12 aryl, C7-18 aralkyl, 6- to 15-membered heteroaralkyl and 6- to 12-membered heterocyclylalkyl wherein each of these groups are optionally substituted with from one to three optional substituents; R2 is selected from CF3, O-C(O)-R6, C(O)R7, C(O)NHR7 and NHC(O)R7; R3 is selected from H, F, CI, Br, I, OH, C1-6 alkyl, OC1-6 alkyl, CH2F, CHF2, CF3, CN, NO2, CO2R8, C(O)NHR10, NHC(O)R10, (CH2)z-NR8R9 and (CH2)z-NH-C(=NH)-NH2; R4 is selected from H, C1-6 alkyl and CH2R11; R5 is selected from C1-6 alkyl; R6 is selected from H and C1-6 alkyl; R7 is selected from 5 to 9-membered heteroaryl groups, and phenyl wherein these groups are optionally substituted with from one to three optional substituents; and wherein the heteroaryl group is attached to the rest of compound of formula (I) by a carbon ring atom; R8 and R9 are independently selected from H, C1-6 alkyl and benzyl; R10 is selected from 5- to 9-membered heteroaryl groups, 5- and 6-membered heterocyclyl, and phenyl wherein these groups are optionally substituted with from one to three optional substituents; R11 is phenyl optionally substituted; and z is selected from an integer selected from o to 6.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H165N | ChemSpider