Category: quinuclidine

Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. 707-37-9, Name is 1-Hydroxy-3,5-dimethyladamantane, molecular formula is C12H20O, belongs to quinuclidine compound, is a common compound. In a patnet, author is Dolle, F, once mentioned the new application about 707-37-9, SDS of cas: 707-37-9.

The lead compound of a new series of azabicyclic carbamates described by Astra Laboratories as ligands for the alpha7 nicotinic acetylcholine receptor subtype, namely N-(4-bromophenyl)carbamic acid quinuclidin-3-yl ester, has been labelled with carbon-11 using no-carrier-added [C-11]phosgene and the isocyanate pathway. Typically, 25-35 mCi (0.92-1.29 GBq) of the tracer was obtained within 30 min of radiosynthesis (HPLC purification included) with specific radioactivities ranging from 500 to 800 mCi/mu mol (18.5-29.6 GBq/mu mol). Biodistribution studies demonstrated a relatively good brain uptake of the compound (0.8-1.2% I.D./g tissue in various brain regions), but without preferential concentration in brain regions rich in alpha7-subtype nicotinic receptor (e.g. hippocampus, pons and colliculi). No specific binding could be demonstrated in pre-saturation studies performed with both the cold compound and nicotine. Therefore, this ligand is not suitable for further exploration in PET imaging. Copyright (C) 2001 John Wiley & Sons, Ltd.

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.Interested yet? Keep reading other articles of 707-37-9, you can contact me at any time and look forward to more communication. SDS of cas: 707-37-9.

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Quinuclidine – Wikipedia,
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Application of 294-62-2, Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. 294-62-2, Name is Cyclododecane, SMILES is C1CCCCCCCCCCC1, belongs to quinuclidine compound. In a article, author is Ohtake, A, introduce new discover of the category.

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.

Application 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.

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Quinuclidine – Wikipedia,
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Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings, and research on the structure and performance of functional materials. 142-45-0, Name is Acetylenedicarboxylic Acid, SMILES is O=C(C#CC(O)=O)O, belongs to quinuclidine compound. In a document, author is Karolyi, Benedek Imre, introduce the new discover, Recommanded Product: Acetylenedicarboxylic Acid.

Acylated mono-, bis- and tris- Cinchona-Based Amines Containing Ferrocene or Organic Residues: Synthesis, Structure and in Vitro Antitumor Activity on Selected Human Cancer Cell Lines

A series of novel functionalized mono-, bis-and tris-(S)-{[(2S,4R,8R)-8-ethyl-quinuclidin-2-yl](6-methoxyquinolin-4-yl)}methanamines including ferrocene-containing derivatives was obtained by the reaction of the precursor amine with a variety of acylation agents. Their in vitro antitumor activity was investigated against human leukemia (HL-60), human neuroblastoma (SH-SY5Y), human hepatoma (HepG2) and human breast cancer (MCF-7) cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)-assay and the 50% inhibitory concentration (IC50) values were determined. Our data indicate that the precursor amine has no antitumor activity in vitro, but the bis-methanamines with ureido-, thioureido and amide-type linkers display attractive in vitro cytotoxicity and cytostatic effects on HL-60, HepG2, MCF-7 and SH-SY5Y cells. Besides H-1- and C-13-NMR methods the structures of the new model compounds were also studied by DFT calculations.

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.Interested yet? Keep reading other articles of 142-45-0, you can contact me at any time and look forward to more communication. Recommanded Product: Acetylenedicarboxylic Acid.

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Quinuclidine – Wikipedia,
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In homogeneous catalysis, catalysts are in the same phase as the reactants. Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction.7779-30-8, Name is 1-(2,6,6-Trimethylcyclohex-2-en-1-yl)pent-1-en-3-one, SMILES is CCC(/C=C/C1C(C)=CCCC1(C)C)=O, belongs to quinuclidine compound. In a document, author is Zhou, Rong, introduce the new discover, Recommanded Product: 1-(2,6,6-Trimethylcyclohex-2-en-1-yl)pent-1-en-3-one.

Visible-Light-Mediated Metal-Free Hydrosilylation of Alkenes through Selective Hydrogen Atom Transfer for Si-H Activation

Although there has been significant progress in the development of transition-metal-catalyzed hydrosilylations of alkenes over the past several decades, metal-free hydrosilylation is still rare and highly desirable. Herein, we report a convenient visible-light-driven metal-free hydrosilylation of both electron-deficient and electron-rich alkenes that proceeds through selective hydrogen atom transfer for Si-H activation. The synergistic combination of the organophotoredox catalyst 4CzIPN with quinuclidin-3-yl acetate enabled the hydrosilylation of electron-deficient alkenes by selective Si-H activation while the hydrosilylation of electron-rich alkenes was achieved by merging photoredox and polarity-reversal catalysis.

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.Interested yet? Keep reading other articles of 7779-30-8, you can contact me at any time and look forward to more communication. Recommanded Product: 1-(2,6,6-Trimethylcyclohex-2-en-1-yl)pent-1-en-3-one.

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Quinuclidine – Wikipedia,
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Related Products of 4430-31-3, In homogeneous catalysis, catalysts are in the same phase as the reactants. Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 4430-31-3, Name is Octahydro-2H-chromen-2-one, SMILES is O=C1CCC2CCCCC2O1, belongs to quinuclidine compound. In a article, author is Liu, H, introduce new discover of the category.

Synthesis and crystal structure of quinuclidin-3-yl 2-cyclopentyl-2-hydroxy-2-phenylacetate

Quinuclidin-3-yl 2-cyclopentyl-2-hydroxy-2-phenylacetate, a more effective the muscarinic receptor antagonist, was synthesised and its crystal structure was first elucidated by X-ray crystallography.

Related Products of 4430-31-3, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 4430-31-3 is helpful to your research.

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Quinuclidine – Wikipedia,
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In homogeneous catalysis, catalysts are in the same phase as the reactants. Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction.99-67-2, Name is 2-Allylpent-4-enoic acid, SMILES is C=CCC(CC=C)C(O)=O, belongs to quinuclidine compound. In a document, author is Sonar, Vijayakumar N., introduce the new discover, Application In Synthesis of 2-Allylpent-4-enoic acid.

Novel substituted (Z)-2-(N-benzylindol-3-ylmethylene)-quinuclidin-3-one and (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)-quinuclidin-3-ol derivatives as potent thermal sensitizing agents

Use of ionizing radiation is essential for the management of many human cancers, and therapeutic hyperthermia has been identified as a potent radio sensitizer. Radiation therapy combined with adjuvant hyperthermia represents a potential too] to provide outstanding local-regional control for refractory disease. (Z)-(+/-)-2-(N-Benzylindol-3-ylmethylene)quinuclidin-3-oI (2) and (Z)-(+/-)-2-(N-benzenesulfonylindol-3-ylmethylene)quinuclidin-3-ol (4) were initially identified as potent thermal sensitizers that could lower the threshold needed for thermal sensitivity to radiation treatment. To define the structural requirements of the molecule that are essential for thermal sensitization, we have synthesized and evaluated a series of (Z)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-one (9), and (Z)-()-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-oI (10) analogs that incorporate a variety of substituents in both the indole and N-benzyl moieties. These systematic structure-activity relationship (SAR) studies were designed to further the development and optimization of potential clinically useful thermal sensitizing agents. The most potent analog was compound 10 (R-1 = H, R 2 = 4-Cl), which potently inhibited (93% inhibition at 50 mu M) the growth of HT-29 cells after a 41 degrees C/2 h exposure. (c) 2007 Elsevier Ltd. All rights reserved.

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.If you’re interested in learning more about 99-67-2. The above is the message from the blog manager. Application In Synthesis of 2-Allylpent-4-enoic acid.

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Quinuclidine – Wikipedia,
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Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. 156028-26-1, Name is 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone, molecular formula is C24H4Cl4O6, belongs to quinuclidine compound, is a common compound. In a patnet, author is Ishihara, T, once mentioned the new application about 156028-26-1, Safety of 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone.

Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: Enzyme inhibition and effects on plasma lipid levels

Squalene synthase (E.C. 2.5.1.21) is a microsomal enzyme which catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene, and is involved in the first committed step in cholesterol biosynthesis. It is an attractive target for hypocholesterolemic and hypotriglyceridemic strategies. We synthesized a series of 3-ethylidenequinuclidine derivatives, and evaluated their ability to inhibit squalene synthase in vitro and to lower non-HDL cholesterol levels in hamsters. 3-Ethylidene-quinuclidine derivatives incorporating an unsubstituted 9H-carbazole moiety reduced plasma non-HDL cholesterol levels and did not affect plasma transaminase levels, indicating a lack of hepatotoxicity. Among the novel Compounds, (Z)-2-[2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 8 (YM-53579) and (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 28 (YM-53601) were potent inhibitors of squalene synthase derived from human hepatoma cells, with IC50 Values Of 160 and 79 nM. respectively. They also reduced plasma non-HDL cholesterol levels in hamsters by approximately 50 and 70%, respectively. at all oral dose of 50 mg/kg/day for 5 days. (C) 2003 Elsevier Ltd. All rights reserved.

Enzymes are biological catalysts that produce large increases in reaction rates.Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 156028-26-1, Safety of 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone.

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Quinuclidine – Wikipedia,
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Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, Like 116-31-4, Name is trans-Retinal. In a document, author is Visser, TJ, introducing its new discovery. Formula: https://www.ambeed.com/products/116-31-4.html.

Stereoselective synthesis and biodistribution of potent [C-11]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways

Quantitation of muscarinic receptors in the lungs in vivo with positron emission tomography (PET) is of clinical interest. For that purpose we decided to develop [C-11]-labeled ligands with a high affinity (K-D < 0.1 nM). Three quaternary muscarinic antagonists, racemic N-methylpiperidin-4-yl 2-cyclohexy-2-2-hydroxy-2-phenylacetate methiodide 1a (pK(B) = 10.39), its (R)-isomer 1b (pK(B) = 11.08), and (R,R)-quinuclidin-3-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate methiodide 2 (pK(B) = 11.28), were labeled by reacting [C-11]CH3I With their tertiary amine precursors. The enantiomerically pure tertiary amine precursors were prepared by stereoselective synthesis starting from (R)-(-)-mandelic acid. In vitro binding assay of 1b and 2 demonstrated that both ligands bind with very high affinity to the muscarinic receptor subtypes M(1), M(2), and M(3). They are more potent than the muscarinic antagonist (R)-N-methylquinuclidinyl benzilate ((R)-MQNB). Distribution studies with la, 1b, and 2 in control and atropine-treated male Wistar rats demonstrated significant specific binding (90-99% of total issue uptake) in tissues containing cholinoceptors (heart, intestine, lung, pancreas, spleen, stomach, submandibular gland). Because the tissue/plasma concentration ratios of 1b are most favorable, this ligand was used for further evaluation. Analysis of plasma samples showed a very rapid clearance (t(1/2) = 0.3 min) of the radioligand 1b and a relatively slow appearance of a hydrophilic metabolite. At 15 min postinjection of 1b, analysis of heart, lungs, and liver showed that respectively 99%, 88%, and 8% of the tissue radioactivity corresponded with the parent compound. Ligand 1b appears to be an excellent candidate for PET studies of mAChR receptors in heart and lungs. 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.Interested yet? Keep reading other articles of 116-31-4, you can contact me at any time and look forward to more communication. Formula: https://www.ambeed.com/products/116-31-4.html.

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Quinuclidine – Wikipedia,
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Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, Like 502-49-8, Name is Cyclooctanone. In a document, author is Tang, Cuyue, introducing its new discovery. SDS of cas: 502-49-8.

Neuropharmacokinetics of two investigational compounds in rats: Divergent temporal profiles in the brain and cerebrospinal fluid

Two investigational compounds (FRM-1, (R)-7-fluoro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and FRM-2, (R)-7-cyano-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide) resided in rat brain longer than in systemic circulation. In Caco-2 directional transport studies, they both showed good intrinsic passive permeability but differed significantly in efflux susceptibility (efflux ratio of <2 and similar to 7, respectively), largely attributed to P-glycoprotein (P-gp). Capitalizing on these interesting properties, we investigated how cerebrospinal fluid (CSF) concentration (C-CSF) would be shaped by unbound plasma concentration (C-u,C-p) and unbound brain concentration (C-u,C-b) in disequilibrium conditions and at steady state. Following subcutaneous administration, FRM-1 C-CSF largely followed C-u,C-p initially and leveled between C-u,C-p and C-u,C-b. However, it gradually approached C-u,C-b and became lower than, but parallel to C-u,C-b at the terminal phase. In contrast, FRM-2 C-CSF temporal profile mostly paralleled the C-u,C-p but was at a much lower level. Upon intravenous infusion to steady state, FRM-1 C-CSF and C-u,C-b were similar, accounting for 61% and 69% of the Cu, indicating a case of largely passive diffusion-governed brain penetration where C-CSF served as a good surrogate for C-u,C-b. On the contrary, FRM-2 C-CSF and C-u,C-b were remarkably lower than C-u,C-p, (17% and 8% of C-u,C-p respectively), suggesting that FRM-2 brain penetration was severely impaired by P-gp-mediated efflux and C-CSF underestimated this impact. A semi-physiologically based pharmacokinetic (PBPK) model was constructed that adequately described the temporal profiles of the compounds in the plasma, brain and CSF. Our work provided some insight into the relative importance of blood-brain barrier (BBB) and blood-CSF barrier (BCSFB) in modulating CCSF. (C) 2014 Elsevier Inc. All rights reserved. Because enzymes can increase reaction rates by enormous factors, typically producing only a single product in quantitative yield, they are the focus of active research.In my other articles, you can also check out more blogs about 502-49-8. SDS of cas: 502-49-8.

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Quinuclidine – Wikipedia,
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Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, Like 112-44-7, Name is Undecanal. In a document, author is Kobayashi, S, introducing its new discovery. Recommanded Product: 112-44-7.

Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: a Ca2+ mobilization study in monkey cells

We investigated the effects of the new muscarinic receptor antagonist solifenacin succinate [YM905; (+)(IS,3′ R)-quinuclidin-3′ -yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] and the current antimuscarinic drugs for the treatment of overactive bladder (oxybutynin, tolterodine and darifenacin) on intracellular Ca2+ mobilization in response to M-3 muscarinic receptor activation in bladder smooth muscle and submandibular gland cells isolated from Cynomolgus monkeys. Solifenacin concentration-dependently inhibited carbachol-induced Ca2+ mobilization, with affinity constant values (pKi) of 8.5+/-0.053 in bladder smooth muscle cells and 8.2+/-0.051 in submandibular gland cells (n=5). The pKi value of solifenacin was almost equivalent to the values of oxybutynin, tolterodine and darifenacin in bladder smooth muscle cells (8.7, 8.5 and 8.4, respectively), while being lower than those in submandibular gland cells (9.0, 8.7 and 8.8, respectively). The bladder-selectivity index (Ki ratio: submandibular gland/bladder) for solifenacin (2.1) was statistically higher, moreover, than those for oxybutynin, tolterodine and darifenacin (0.51, 0.65 and 0.46, respectively). These findings consequently indicate solifenacin’s unique profile in terms of its selectivity for bladder smooth muscle cells over salivary gland cells in non-human primates, relative to oxybutynin, tolterodine and darifenacin. Solifenacin may, therefore, confer a promising therapeutic advantage for reducing adverse effects, such as dry mouth, exhibited by current antimuscarinic therapy for overactive bladder. (C) 2003 Elsevier Inc. All rights reserved.

Enzymes are biological catalysts that produce large increases in reaction rates.Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 112-44-7, Recommanded Product: 112-44-7.

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Quinuclidine – Wikipedia,
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