Archives for Chemistry Experiments of Related Products of 827-61-2

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Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome

Serotonin type 3 (5-HT3) receptor partial agonists are being targeted as potential new drugs for the treatment of irritable bowel syndrome (IBS). Two new chemical series bearing indazole and indole cores have exhibited nanomolar binding affinity for the h5-HT3A receptor. A range of partial agonist activities in HEK cells heterologously expressing the h5-HT 3A receptor were measured for the indazole series. Excellent 5-HT3 receptor selectivity, favorable in vitro metabolic stability and CYP inhibition properties, and good oral in vivo potency in the murine von Bezold-Jarisch reflex model is exemplified thereby indicating the series to have potential utility as improved IBS agents.

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Quinuclidine | C7H150N | ChemSpider

Some scientific research about (R)-3-Aminoquinuclidine dihydrochloride

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NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Compounds of formula (I), wherein D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

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Quinuclidine | C7H106N | ChemSpider

Awesome and Easy Science Experiments about Quinuclidin-3-yl acetate

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Related Products of 827-61-2, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. Related Products of 827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Article, authors is Pasturenzi£¬once mentioned of Related Products of 827-61-2

Thermochemical stability: A comparison between experimental and predicted data

The first step to be performed during the development of a new industrial process should be the assessment of all hazards associated to the involved compounds. Particularly, the knowledge of all substances thermochemical parameters is a primary feature for such a hazard evaluation. CHETAH (CHEmical Thermodynamic And Hazard evaluation) is a prediction software suitable for calculating potential hazards of chemicals, mixtures or a single reaction that, using only the structure of the involved molecules and Benson’s group contribution method, is able to calculate heats of formation, entropies, Gibbs free energies and reaction enthalpies. Because of its ability to predict the potential hazards of a material or mixture, CHETAH is part of the so-called “desktop methods” for early stage chemical safety analysis. In this work, CHETAH software has been used to compile a complete risk database reporting heats of decomposition and Energy Release Potential (ERP) for 342 common use chemicals. These compounds have been gathered into classes depending on their functional groups and similarities in their thermal behavior. Calculated decomposition enthalpies for each of the compounds have also been compared with experimental data obtained with either thermoanalytic or calorimetric techniques (Differential Scanning Calorimeter – DSC – and Accelerating Rate Calorimeter – ARC).

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A new application about 123536-14-1

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NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Compounds of formula (I), wherein D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

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Related Products of 827-61-2, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. Related Products of 827-61-2, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article, authors is Mould, Daniel P.£¬once mentioned of Related Products of 827-61-2

Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1

Inhibition of lysine specific demethylase 1 (LSD1) has been shown to induce the differentiation of leukemia stem cells in acute myeloid leukemia (AML). Irreversible inhibitors developed from the nonspecific inhibitor tranylcypromine have entered clinical trials; however, the development of effective reversible inhibitors has proved more challenging. Herein, we describe our efforts to identify reversible inhibitors of LSD1 from a high throughput screen and subsequent in silico modeling approaches. From a single hit (12) validated by biochemical and biophysical assays, we describe our efforts to develop acyclic scaffold-hops from GSK-690 (1). A further scaffold modification to a (4-cyanophenyl)glycinamide (e.g., 29a) led to the development of compound 32, with a Kd value of 32 nM and an EC50 value of 0.67 muM in a surrogate cellular biomarker assay. Moreover, this derivative does not display the same level of hERG liability as observed with 1 and represents a promising lead for further development.

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Quinuclidine | C7H151N | ChemSpider

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Synthetic Route of 827-61-4, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. Synthetic Route of 827-61-4, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article, authors is Ouach, Aziz£¬once mentioned of Synthetic Route of 827-61-4

Design of alpha7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies

We report here the synthesis of a large library of 1,2,3-triazole derivatives which were in vitro tested as alpha7 nAchR ligands. The SAR study revealed that several crucial factors are involved in the affinity of these compounds for alpha7 nAchR such as a (R) quinuclidine configuration and a mono C-3 quinuclidine substitution. The triazole ring was substituted by a phenyl ring bearing small OMe/CH2F groups or fluorine atom and by several heterocycles such as thiophenes, furanes, benzothiophenes or benzofuranes. Among the 30 derivatives tested, the two derivatives 10 and 39 with Ki in the nanomolar range were identified (2.3 and 3 nM respectively). They exhibited a strict selectivity toward the alpha4beta2 nicotinic receptor (up to 1 muM) but interacted with the 5HT3 receptors with Ki around 3 nM. Synthesis, SAR studies and a full description of the derivatives are reported.

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Quinuclidine | C7H152N | ChemSpider

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, Synthetic Route of 827-61-3, molecular formula is C8H16N2, introducing its new discovery. Synthetic Route of 827-61-3

CEPHEM DERIVATIVE HAVING CATECHOL GROUP

A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.

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Simple exploration of Quinuclidin-3-yl acetate

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Synthetic Route of 827-61-2, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 827-61-2, molcular formula is C9H15NO2, introducing its new discovery.

Muscarinic effects on cellular functions in cultured human ciliary muscle cells

Purpose. To characterize the pharmacology of the carbachol-induced changes of phospholipase C (PLC) activity and intracellular calcium concentration ([Ca2+](i)) in cultured human ciliary muscle cells. Methods. Changes in PLC activity of cultured human ciliary muscle cells were determined by production of inositol phosphates. Single-cell dynamic fluorescence ratio imaging was used to determine [Ca2+](i). Results. Carbachol, oxotremorine-M, aceclidine, and pilocarpine stimulated PLC with mean EC50s of 20, 8, 17, and 2 muM, respectively. The effect of carbachol on PLC was partially suppressed by extracellular Ca2+ depletion. This muscarinic effect was blocked by muscarinic antagonists, such as atropine (apparent pK(i) = 9.12, nonselective for muscarinic receptor subtypes), pirenzepine (pK(i) = 6.76, selective for the M1 receptor subtype), 4DAMP (pK(i) = 9.25, selective for the M1 and M3 subtypes), and fHHSiD (pK(i) = 7.77, selective for the M3 subtype). In [Ca2+](i) experiments, carbachol increased [Ca2+](i) transients in human ciliary muscle cells in a dose-dependent manner with a mean EC50 of 7 muM. 4DAMP was approximately 100 times more potent than pirenzepine in the inhibition of the carbachol-induced [Ca2+](i) increase. [Ca2+](i) oscillations were observed after carbachol stimulation and persisted after extracellular Ca2+ depletion. Conclusions. Muscarinic agonists activate PLC and increase [Ca2+](i) in cultured human ciliary muscle cells through an M3-like muscarinic receptor subtype.

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TREATMENT OF SEXUAL DYSFUNCTION AND FOR IMPROVED SEXUAL QUALITY OF LIFE

Compositions and methods for treating sexual dysfunction and enhancing sexual satisfaction using topical application of alpha-1 adrenergic receptor agonists, muscarinic acetylcholine receptor agonists, nicotinic acetylcholine receptor agonists, and cholinesterase inhibitors are disclosed.

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New explortion of (R)-3-Aminoquinuclidine dihydrochloride

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Synthesis of combinatorial libraries of compounds reminiscent of natural products

The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

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Quinuclidine | C7H131N | ChemSpider