Category: quinuclidine

Application of 13419-61-9, 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. 13419-61-9, Name is Sodium decane-1-sulfonate, SMILES is CCCCCCCCCCS(=O)([O-])=O.[Na+], belongs to quinuclidine compound. In a article, author is Dolle, F, introduce new discover of the category.

Highly efficient synthesis of [C-11]Me-QNB, a selective radioligand for the quantification of the cardiac muscarinic receptors using PET

Me-QNB (N-methyl-quinuclidin-3-yl benzilate or N-methyl-quinuclidin-3-yl diphenylhydroxy acetate) is a hydrophilic, non-metabolized and highly specific muscarinic acetylcholinergic antagonist. Using this quaternary ammonium derivative of QNB, labelled with carbon-11, a positron-emitting isotope (half-life : 20.4 minutes), the potential for quantification of myocardial muscarinic receptors in vivo using the high-resolution, sensitive and quantitative imaging technique PET (positron emission tomography) was previously demonstrated in dogs and validated in humans. In this paper, the radiosynthesis of carbon-11-labelled Me-QNB is investigated and oriented towards the preparation of multi milliCuries of radiotracer. Typically, using no-carrier-added [C-11]methyl triflate as the alkylating agent and 0.64 mg (1.89 mu mol) of QNB as precursor for labelling at 100 degreesC for 1 minute lead to a 48.5% +/- 10% (15 runs) decay-corrected radiochemical yield (based on [C-11]methyl triflate). 183 mCi (+/- 39) of [C-11]Me-QNB ([C-11]-1) could be synthesized in only 27 to 28 minutes after EOB and occasionally, up to 340 mCi of [C-11]Me-QNB ([C-11]-1) were obtained, corresponding to a 85% decay-corrected yield. The associated decay-corrected specific radioactivities obtained were 2658 mCi/mu mol (+/- 971) at EOB.

Application of 13419-61-9, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 13419-61-9.

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Quinuclidine – Wikipedia,
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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner.In an article, author is Naito, Ryo, once mentioned the application of 871-91-0, Name is 7-Octyn-1-ol, molecular formula is C8H14O, molecular weight is 126.2, MDL number is MFCD01632137, category is quinuclidine. Now introduce a scientific discovery about this category, Category: quinuclidines.

Research and Development of Solifenacin for the Treatment of Overactive Bladder (OAB)

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.

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 871-91-0. Category: quinuclidines.

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Electric Literature of 611-10-9, Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. 611-10-9, Name is Ethyl 2-oxocyclopentanecarboxylate, SMILES is C(OC(C1C(CCC1)=O)=O)C, belongs to quinuclidine compound. In a article, author is Brown, GR, introduce new discover of the category.

Novel optimised quinuclidine squalene synthase inhibitors

Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol 1c, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral ED(50) of 1c, for the inhibition of rat cholesterol biosynthesis was 1.3+/-0.45 mg/kg and for the R-enantiomer 1m, 0.8+/-0.2 mg/kg, with the corresponding R-carboxylic acid 6a, being 0.9+/-0.25 mg/kg. (C) 1997 Elsevier Science Ltd. All rights reserved.

Electric Literature of 611-10-9, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 611-10-9.

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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.301-02-0, Name is Oleamide, SMILES is CCCCCCCC/C=CCCCCCCCC(N)=O, belongs to quinuclidine compound. In a document, author is Odzak, R, introduce the new discover, Recommanded Product: Oleamide.

3-Amidoquinuclidine derivatives: Synthesis of compounds and inhibition of butyrylcholinesterase

The synthesis of racemic and enantiomerically pure 3-butanamidoquinuclidines ((+/-)-Bu, (R)-Bu and (S)-Bu), (1-3) and 3-benzamidoquinuclidines ((+/-)-Bz, (R)-Bz, and (S)-Bz), (4-6) is described. The N-quaternary derivatives, N-benzyl-3-butatiamidoquinuclidinium bromides ((+/-)-Bn1Bu, (R)-Bn1Bu and (S)-Bn1Bu), (7-9) and N-betizyl-3-beiizaimidoquinuclidiniuim bromides ((+/-)-Bn1Bz, (R)-Bn1Bz and (S)-Bn1Bz), (10-12) were subsequently synthesized. The interaction of the four enantiomerically pure quaternary derivatives with horse serum butyrylcholinesterase (BChE) was tested. All tested Compounds inhibited the enzyme. The best inhibitior of the enzyme was (S)-Bn1Bz with a K-i = 3.7 mu M. The inhibitor potency decreases in order (S)-Bn1Bz > (R)-Bn1Bz > (R)-Bn1Bu > (S)Bn1Bu. (c) 2006 Elsevier Inc. All rights reserved.

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 301-02-0, you can contact me at any time and look forward to more communication. Recommanded Product: Oleamide.

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Quinuclidine – Wikipedia,
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Electric Literature of 7779-30-8, Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. 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 article, author is Lima, Fabio, introduce new discover of the category.

A Lewis Base Catalysis Approach for the Photoredox Activation of Boronic Acids and Esters

We report herein the use of a dual catalytic system comprising a Lewis base catalyst such as quinuclidin-3-ol or 4-dimethylaminopyridine and a photoredox catalyst to generate carbon radicals from either boronic acids or esters. This system enabled a wide range of alkyl boronic esters and aryl or alkyl boronic acids to react with electron-deficient olefins via radical addition to efficiently form C-C coupled products in a redox-neutral fashion. The Lewis base catalyst was shown to form a redox-active complex with either the boronic esters or the trimeric form of the boronic acids (boroxines) in solution.

Electric Literature of 7779-30-8, 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 7779-30-8.

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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 765-70-8, Name is 3-Methylcyclopentane-1,2-dione. In a document, author is Herschorn, Sender, introducing its new discovery. Category: quinuclidines.

Tolerability of 5 mg Solifenacin Once Daily Versus 5 mg Oxybutynin Immediate Release 3 Times Daily: Results of the VECTOR Trial

Purpose: Although antimuscarinic treatment is indicated for overactive bladder, many patients discontinue it because of dry mouth. Of available antimuscarinics oxybutynin is associated with the highest dry mouth rate. We compared the safety and tolerability of 5 mg solifenacin vs 15 mg oxybutynin immediate release. Materials and Methods: At 12 Canadian centers a total of 132 patients with overactive bladder symptoms (greater than 1 urgency episode per 24 hours, and 8 or greater micturitions per 24 hours) were randomized to 5 mg solifenacin once daily or 5 mg oxybutynin 3 times daily for 8 weeks. The primary end point was the incidence and severity of dry mouth reported after direct questioning. Efficacy end points (3-day diary documented changes in urgency, frequency, incontinence, nocturia and voided volume), and changes on the Patient Perception of Bladder Condition scale and the Overactive Bladder Questionnaire were evaluated secondarily. Results: Of patients on solifenacin vs oxybutynin immediate release 35% vs 83% reported dry mouth (p <0.0001). Of patients reporting dry mouth severity was graded moderate by 13% and 42% of those on solifenacin and oxybutynin immediate release, and severe by 13% and 28%, respectively (p = 0.001). Patients in each group showed improvements in efficacy end points, and Patient Perception of Bladder Condition scale and Overactive Bladder Questionnaire scores from baseline to treatment end. Conclusions: Significantly fewer patients on 5 mg solifenacin once daily reported dry mouth vs those receiving 5 mg oxybutynin immediate release 3 times daily. Significantly fewer patients on solifenacin reported moderate/severe dry mouth. Significantly fewer patients on solifenacin withdrew from study due to dry mouth and there were significantly fewer overall adverse events. Solifenacin and oxybutynin immediate release were efficacious in decreasing efficacy end points, and improved Patient Perception of Bladder Condition scale and Overactive Bladder Questionnaire results from baseline to treatment end. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. 765-70-8, you can contact me at any time and look forward to more communication. Category: quinuclidines.

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Quinuclidine – Wikipedia,
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This type of reactivity has quickly become one of the cornerstones of modern catalysis. The transformation of simple hydrocarbons into more complex products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 502-49-8, Name is Cyclooctanone. In a pantent, once mentioned the new application about 502-49-8, Recommanded Product: 502-49-8.

3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione for circumvention of anticancer drug resistance

A series of 3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3 -f]indole-5,10-dione was synthesized by Mannich reaction or by the transamination of 3-dimethylaminomethyl 4,11-dihydroxy- or 4,11-dimethoxynaphtho[2,3-f]indole-5,10-dione. The potency of novel derivatives was tested on a National Cancer Institute panel of 60 human tumor cell lines as well as in cells with genetically defined determinants of cytotoxic drug resistance, P-glycoprotein (Pgp) expression, and p53 inactivation. Mannich derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione with an additional amino function in their side chain, demonstrated equal cytotoxicity against the parental K562 leukemia cells and their Pgp-positive subline, whereas the latter showed similar to 7-fold resistance to adriamycin, a Pgp transported drug. 3-(1-Piperazinyl)methyl and 3-(quinuclidin-3-yl)aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione killed HCT116 colon carcinoma cells (carrying wild type p53) and their p53-null variant within the similar range of concentrations. We conclude that Mannich modification of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione, especially when cyclic diamine (e.g., piperazine, quinuclidine) is used, confers an important feature to the resulting compounds, namely, the potency for tumor cells otherwise resistant to a variety of anticancer drugs. (c) 2004 Elsevier Ltd. All rights reserved.

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.Interested yet? Keep reading other articles of 502-49-8, you can contact me at any time and look forward to more communication. Recommanded Product: 502-49-8.

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Quinuclidine – Wikipedia,
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As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. Safety of Methyl oleate, 112-62-9, Name is Methyl oleate, SMILES is CCCCCCCC/C=CCCCCCCCC(OC)=O, in an article , author is Ohtake, A, once mentioned of 112-62-9.

In vitro and in vivo tissue selectivity profile of solifenacin succinate (YM905) for urinary bladder over salivary gland in rats

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.

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 112-62-9. The above is the message from the blog manager. Safety of Methyl oleate.

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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. 5324-84-5, Name is Sodium octane-1-sulfonate, molecular formula is C8H17NaO3S, belongs to quinuclidine compound, is a common compound. In a patnet, author is Tudosie, Mihail S., once mentioned the new application about 5324-84-5, Computed Properties of C8H17NaO3S.

New synthesized oximes active in nerve agents’ hazards

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.

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 5324-84-5, Computed Properties of C8H17NaO3S.

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Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 142-45-0, Name is Acetylenedicarboxylic Acid, SMILES is O=C(C#CC(O)=O)O, in an article , author is Trost, BM, once mentioned of 142-45-0, Name: Acetylenedicarboxylic Acid.

Intramolecular palladium-catalyzed allylic alkylation: Enantio- and diastereoselective synthesis of [2.2.2] bicycles

[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.

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. Name: Acetylenedicarboxylic Acid.

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