Month: July 2021

Computed Properties of https://www.ambeed.com/products/1120-72-5.html, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 1120-72-5, Name is 2-Methylcyclopentan-1-one, SMILES is O=C1C(C)CCC1, belongs to quinuclidine compound. In a article, author is Ugawa, T, introduce new discover of the category.

1 To better understand how it decreases plasma cholesterol and triglyceride levels, we evaluated the effect of (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole monohydrochloride (YM-53601) on lipogenic biosynthesis in the liver and lipid secretion from the liver in rats and hamsters. 2 Single administration of YM-53601 in cholestyramine-treated rats inhibited triglyceride and free fatty acid (FFA) biosynthesis at a similar dose range to that at which it inhibited cholesterol biosynthesis. YM-53601 inhibited both triglyceride and FFA biosynthesis in hamsters treated with cholestyramine. 3 YM-53601 by single oral administration decreased the enhanced plasma triglyceride levels in hamsters induced by an injection of protamine sulfate, which inhibits lipoprotein lipase (LPL) and consequently increases plasma very low-density lipoprotein (VLDL) triglyceride levels. YM-53601 also decreased the enhanced plasma triglyceride and cholesterol levels in hamsters treated with Triton WR1339, which also inhibits the degradation of VLDL. Plasma cholesterol was significantly decreased as soon as I h after single administration of YM-53601 in hamsters fed a normal diet. 4 This is the first report that a squalene synthase inhibitor suppresses lipogenic biosynthesis in the liver and cholesterol and triglyceride secretion from the liver in vivo. We therefore suggest that the mechanism by which YM-53601 decreases plasma triglyceride might include these effects. The finding that YM-53601 rapidly decreased plasma cholesterol suggests that this compound may be effective in decreasing plasma cholesterol levels early in the course of treatment of hypercholesterotemia in humans.

Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly. You can get involved in discussing the latest developments in this exciting area about 1120-72-5. Computed Properties of https://www.ambeed.com/products/1120-72-5.html.

Reference:
Quinuclidine – Wikipedia,
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Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. 2756-87-8, Name is (E)-4-methoxy-4-oxobut-2-enoic acid. In a document, author is Naito, Ryo, introducing its new discovery. HPLC of Formula: https://www.ambeed.com/products/2756-87-8.html.

Solifenacin succinate (Vesicare (R)), a novel muscarinic receptor antagonist for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency, has been approved in more than 60 countries. In the course of continuing efforts to develop potent and bladder-selective muscarinic M-3 receptor antagonists, solifenacin was designed as one of conformationally restricted analogues of quinuclidin-3-yl benzhydrylcarbamate with little selectivity among muscarinic receptor subtypes. In preclinical studies, solifenacin exhibited a highly bladder-selective profile compared with other antimuscarinic agents. Clinically, solifenacin ameliorates all symptoms in OAB patients; and, in particular, it produces a significant decrease in urgency episodes, which is the principal symptom of OAB with good tolerability. In this article, the drug discovery and the process development of solifenacin succinate are described.

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Reference:
Quinuclidine – Wikipedia,
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Computed Properties of https://www.ambeed.com/products/13139-15-6.html, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 13139-15-6, Name is Boc-L-Leucine, SMILES is CC(C)C[C@H](NC(OC(C)(C)C)=O)C(O)=O, belongs to quinuclidine compound. In a article, author is Ugawa, T, introduce new discover of the category.

1 The aim of this study was to establish an experimental model of the escape phenomenon, in which plasma cholesterol, initially reduced by a 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase inhibitor such as pravastatin, increases again on long-term administration. We also evaluated the efficacy of YM-53601 ((E)-2-[2-fluoro-2- (quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a squalene synthase inhibitor, in this model. 2 Pravastatin inhibited cholesterol biosynthesis in hamster primary hepatocytes (IC50, 14 nM). After pre-treatment with pravastatin, in contrast, almost no effect on cholesterol biosynthesis was seen. 3 In hamsters fed a high fat diet, 3 mg kg(-1) pravastatin for 9 days decreased plasma non-HDL cholesterol (total cholesterol-high density lipoprotein cholesterol) (P<0.01), but this effect was lost between 17 and 27 days of treatment, accompanied by an increase in HMG-CoA reductase activity. No such increase in plasma non-HDL cholesterol was seen with YM-53601 at 30 mg kg(-1) after 9 (P<0.001), 17 (P<0.01) or 27 (P<0.001) days of treatment. Replacement of pravastatin with YM-53601 caused a decrease in plasma non-HDL cholesterol by 53% (P<0.001) and in HMG-CoA reductase activity. 4 This animal model thus satisfactorily replicates the escape phenomenon observed in humans and may therefore be useful in evaluation of lipid-lowering agents, specifically comparison of HMG-CoA reductase inhibitors. Further, YM-53601 may be useful in the treatment of hypercholesterolemia without induction of the escape phenomenon. Computed Properties of https://www.ambeed.com/products/13139-15-6.html, This is the end of this tutorial post, and I hope it has helped your research about 13139-15-6.

Reference:
Quinuclidine – Wikipedia,
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Some examples of the diverse research done by chemistry experts include discovery of new medicines and vaccines, improving understanding of environmental issues, and development of new chemical products and materials Like 6413-10-1, Name is Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate. In a document, author is Naito, R, introducing its new discovery. Reference of 6413-10-1.

A novel series of biphenylylcarbamate derivatives were synthesized and evaluated for binding to M-1, M-2 and M-3 receptors and for antimuscarinic activities. Receptor binding assays indicated that biphenyl-2-ylcarbamate derivatives had high affinities for M-1 and M-3 receptors and good selectivities for M-3 receptor over M-2 receptor, indicating that the biphenyl-2-yl group is a novel hydrophobic replacement for the benzhydryl group in the muscarinic antagonist field. In this series, quinuclidin-1-yl biphenyl-2-ylcarbamate monohydrochloride (81, YM-46303) exhibited the highest affinities for M-1 and M-3 receptors, and selectivity for M-3 over M-2 receptor. Compared to oxybutynin, YM-46303 showed approximately ten times higher inhibitory activity on bladder pressure in reflexly-evoked rhythmic contraction, and about 5-fold greater selectivity for urinary bladder contraction against salivary secretion in rats. Moreover, selective antagonistic activity was also observed in vitro. Further evaluation of antimuscarinic effects on bradycardia and presser in pithed rats, and on tremor in mice, showed that YM-46303 can be useful for the treatment of urinary urge incontinence as a bladder-selective M-3 antagonist with potent activities and fewer side effects.

Reference of 6413-10-1, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 6413-10-1 is helpful to your research.

Reference:
Quinuclidine – Wikipedia,
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New Advances in Chemical Research in 2021.Researchers are common within chemical engineering and are often tasked with creating and developing new chemical techniques, frequently combining other advanced and emerging scientific areas. Like 6753-98-6, Name is (1E,4E,8E)-2,6,6,9-Tetramethylcycloundeca-1,4,8-triene. In a document, author is Tudosie, Mihail S., introducing its new discovery. Application of 6753-98-6.

Object: The aim of the study is to select the most active new imidazolium-quinuclidinumoxime, from some similar chemical compounds synthesized in our chemistry department, with sufficient efficacy to decrease the acute toxicity of neurotoxic organophosphates known as nerve agents. Method: The experimental study consist in vivo testing the antidotal efficacy of obidoxime and of selected imidazolium oximes synthesized in our chemistry department. Each oxime was included, by equimolar replacing the obidoxime, in an antidotal formula, which also contains atropine. The above mentioned formula containing atropine and obidoxime was used as reference. The protective ratio, defined as the ratio between the lethal median dose of the poisoned and treated study group and the median lethal dose (LD50) of the poisoned and untreated study groups was one of the used parameters in order to select a new active chemical structure in counteracting the neurotoxic organophosphorus compounds acute toxicity. Another studied parameter was the erythrocyte acetylcholinesterase value measured in whole blood 24 hours after exposure. Results: The protective ratio against an organophosphorus compound were the follow: obidoxime chloride: 2; 1,3dimethyl-2-hydroxyethyl-imidazolyliodide: 1,75;3-oxime-[3-(2-hidroxyimino-methyl-1-imidazolyl-)-2oxapropyl] quinuclidin-dichl-oride: 2,5; 1-methyl-quinuclidin-3-iodide: 1,5. The erythrocyte acetycholinesterase main values were the following: the unpoisoned and untreated study group: 3,45 +/- 0,13mmol/dl; the poisoned and untreated study group: 0,89 +/- 0,09 mmol/dl; the poisoned and 3oxime-[3-(2-hidroxyimino-methyl-1-imidazolyl-)-2oxapropyl]quinuclidindichloride treated study group: 2,89 +/- 0,11 mmol/dl; the poisoned and obidoxime treated study group: 2,53 +/- 0,15 mmol/dl. Conclusions: 3-oxime-[3-(2-hidroxyimino-methyl-1-imidazolyl-)-2oxapropyl] quinuclidindichloride synthesized in our chemistry department, has shown a better protective ratio and a more prolonged surviving time than the reference (obidoxime). It has shown the best AChE reactivation of all the synthetized compounds. This compound can be a cheap and good option for replacing obidoxime in the antidotal formula active in nerve agent exposure.

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Reference:
Quinuclidine – Wikipedia,
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New Advances in Chemical Research in 2021. Chemistry graduates have much scope to use their knowledge in a range of research sectors, including roles within chemical engineering, chemical and related industries, healthcare and more. Like 1490-25-1, Name is Methyl 4-chloro-4-oxobutanoate. In a document, author is Trost, BM, introducing its new discovery. Application of 1490-25-1.

[GRAPHICS] Pd-catalyzed asymmetric allylic alkylation provides both enantio- and diastereoselectivity in formation of bicyclo [2.2.2] octan-2,3-diones and quinuclidin-2-ones, the latter potential precursors to quinine alkaloids.

Application of 1490-25-1, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 1490-25-1 is helpful to your research.

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Quinuclidine – Wikipedia,
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Some examples of the diverse research done by chemistry experts include discovery of new medicines and vaccines, improving understanding of environmental issues, and development of new chemical products and materials Like 10160-87-9, Name is 3,3-Diethoxyprop-1-yne. In a document, author is Naito, Ryo, introducing its new discovery. Reference of 10160-87-9.

Solifenacin succinate (Vesicare (R)), a novel muscarinic receptor antagonist for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency, has been approved in more than 60 countries. In the course of continuing efforts to develop potent and bladder-selective muscarinic M-3 receptor antagonists, solifenacin was designed as one of conformationally restricted analogues of quinuclidin-3-yl benzhydrylcarbamate with little selectivity among muscarinic receptor subtypes. In preclinical studies, solifenacin exhibited a highly bladder-selective profile compared with other antimuscarinic agents. Clinically, solifenacin ameliorates all symptoms in OAB patients; and, in particular, it produces a significant decrease in urgency episodes, which is the principal symptom of OAB with good tolerability. In this article, the drug discovery and the process development of solifenacin succinate are described.

Reference of 10160-87-9, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 10160-87-9 is helpful to your research.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Academic researchers, R&D teams, teachers, students, policy makers and the media all rely on us to share knowledge that is reliable, accurate and cutting-edge. Like 294-62-2, Name is Cyclododecane. In a document, author is Ohtake, A, introducing its new discovery. Synthetic Route of 294-62-2.

Solifenacin succinate [YM905; (+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The aim of the present study was to evaluate the in vitro and in vivo bladder selectivity profile of solifenacin over salivary gland in the same animal species, and to compare the results with those obtained for tolterodine, oxybutynin, darifenacin and atropine. Solifenacin and the other antimuscarinic drugs inhibited carbachol-induced increases in intracellular Ca2+ levels in bladder smooth muscle cells and salivary gland cells isolated from rats in a concentration-dependent manner. The inhibitory effect of solifenacin for bladder smooth muscle cells (pK(i) = 8.12) was 3.6-fold more potent than that for salivary gland cells (pK(i) = 7.57). In contrast, the inhibitory effects of the other antimuscarinic drugs for bladder smooth muscle cells were 1.7- to 2.2-fold more potent than those for salivary gland cells. In anesthetized rats, solifenacin dose-dependently inhibited carbachol-induced intravesical pressure elevation and salivary secretion, and exhibited functional selectivity (3.7- to 6.5-fold) for urinary bladder over salivary gland. Tolterodine was also 2.2- to 2.4-fold more selective in inhibition of bladder response. In contrast, oxybutynin, darifenacin and atropine did not show functional selectivity for urinary bladder. These results indicate that solifenacin exerts greater selectivity for urinary bladder over salivary gland than tolterodine, oxybutynin, darifenacin and atropine, and may consequently provide symptomatic benefit in the treatment of overactive bladder with less dry mouth than currently used antimuscarinic drugs. (C) 2004 Elsevier B.V. All rights reserved.

Synthetic Route of 294-62-2, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 294-62-2.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

New Advances in Chemical Research in 2021. Chemistry graduates have much scope to use their knowledge in a range of research sectors, including roles within chemical engineering, chemical and related industries, healthcare and more. Like 924-50-5, Name is Methyl-3,3-dimethylacrylate. In a document, author is d’Agostino, Simone, introducing its new discovery. Recommanded Product: 924-50-5.

Condensation reactions between 1,8-naphthalic anhydride and racemic 3-aminoquinuclidine or chiral (S) or (R)-(-)-3-aminoquinuclidine allowed preparation of three novel racemic and enantiopure aza-donor ligands, namely NMiABCO (1), (S)NMiABCO (2a), and (R)NMiABCO (2b). Racemic NMiABCO (1) crystallizes in the monoclinic space group P2(1)/c, Z’ = 1, while enantiopure (S)NMiABCO (2a) and (R)NMiABCO (2b) crystallize in the chiral monoclinic space group P2(1), Z’ = 2, and show significant pseudocentrosymmetry, being pseudo-isomorphous with racemic NMiABCO (1). Reactivity of both racemic and enantiopure NMiABCO toward iodine and interhalogen IBr was also investigated as a way to remove the pseudoisomorphism, yielding the three new molecular adducts [NMiABCO center dot I-2] (3), [(S)NMiABCO center dot I-2]center dot xCHCl(3) (4), [(S)NMiABCO center dot IBr]center dot xCHCl(3) (5) and the molecular salt [HNMIABCO][1Br(2)] (6). Synthesis of complexes 3 and 4 was also carried out in the solid state via kneading and vapor digestion techniques. All compounds were fully characterized via single crystal and powder X-ray diffraction and Raman spectroscopy.

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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

New Advances in Chemical Research in 2021. Chemistry graduates have much scope to use their knowledge in a range of research sectors, including roles within chemical engineering, chemical and related industries, healthcare and more. Like 871-91-0, Name is 7-Octyn-1-ol. In a document, author is Naito, R, introducing its new discovery. Formula: https://www.ambeed.com/products/871-91-0.html.

A novel series of biphenylylcarbamate derivatives were synthesized and evaluated for binding to M-1, M-2 and M-3 receptors and for antimuscarinic activities. Receptor binding assays indicated that biphenyl-2-ylcarbamate derivatives had high affinities for M-1 and M-3 receptors and good selectivities for M-3 receptor over M-2 receptor, indicating that the biphenyl-2-yl group is a novel hydrophobic replacement for the benzhydryl group in the muscarinic antagonist field. In this series, quinuclidin-1-yl biphenyl-2-ylcarbamate monohydrochloride (81, YM-46303) exhibited the highest affinities for M-1 and M-3 receptors, and selectivity for M-3 over M-2 receptor. Compared to oxybutynin, YM-46303 showed approximately ten times higher inhibitory activity on bladder pressure in reflexly-evoked rhythmic contraction, and about 5-fold greater selectivity for urinary bladder contraction against salivary secretion in rats. Moreover, selective antagonistic activity was also observed in vitro. Further evaluation of antimuscarinic effects on bradycardia and presser in pithed rats, and on tremor in mice, showed that YM-46303 can be useful for the treatment of urinary urge incontinence as a bladder-selective M-3 antagonist with potent activities and fewer side effects.

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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider