Category: quinuclidines

141627-42-1, Name is (2-Butyl-5-nitrobenzofuran-3-yl)(4-methoxyphenyl)methanone, molecular formula is C20H19NO5, belongs to quinuclidines compound, is a common compound. In a patnet, author is Primozic, I, once mentioned the new application about 141627-42-1, SDS of cas: 141627-42-1.

Interactions of chiral quinuclidin-3-yl benzoates with butyrylcholinesterase: kinetic study and docking simulations

Both enantiomers of quinuclidin-3-yl benzoate (RQBz and SQBz) were synthesized in order to examine the stereoselectivity of the hydrolysis of these esters catalyzed by horse serum butyrylcholinesterase (BChE). The hydrolysis of benzoylcholine (BzCh) was also studied in order to determine the influence of the alcohol part of the esters upon the kinetics. The k(cat) value for the substrates decreased in order BzCh > RQBz (4-fold slower) much greater than SQBz (76-fold slower reaction). K-M values determined for quinuclidinium substrates revealed that the binding affinity of RQBz (0.28 mm) is approximately 2-fold lower than that of SQBz (0.13 mM) towards BChE. From the ratio of the enantiomeric k(cat)/K-M values, an enantiomeric excess of 78% was calculated, indicating that the resolution of racemic quinuclidin-3-yl benzoate can be achieved by hydrolysis with BChE. The orientations of all the studied benzoate esters and butyrylcholine (BuCh) in the active site of human BChE were proposed by flexible ligand docking with AutoDock 3.0. Analyses of the Michaelis complexes obtained revealed that there are numerous similar close contacts in the active site. The main difference in binding of quinuclidinium and choline esters was found in the ammonium electrostatic region which includes cation-pi interaction of the ammonium moiety of substrates with the indole ring of Trp(84). The important cation-pi interaction with Trp(84) was lowest in the case of the S-enantiomer of QBz, which might be the main explanation for the slowest rate of hydrolysis of that compound. Copyright (C) 2002 John Wiley Sons, Ltd.

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Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 2442-10-6, Name is 1-Octen-3-yl Acetate, molecular formula is , belongs to quinuclidines compound. In a document, author is Ikeda, K, Name: 1-Octen-3-yl Acetate.

M-3 receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland

The antimuscarinic profile of the experimental drug solifenacin/YM905 [(+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate] for the treatment of overactive bladder was compared with the commonly prescribed agent oxybutynin. In radioligand binding assays, pK(i) values of solifenacin for M-1, M-2, and M-3 receptors were 7.6, 6.9, and 8.0, respectively. These values for oxybutynin were 8.6 (M-1), 7.7 (M-2), and 8.9 (M-3). Solifenacin and oxybutynin antagonized the contractile effect of carbachol (CCh) on isolated guinea pig urinary bladder smooth muscle (detrusor), displaying the negative logarithm of antagonist apparent affinity constant (pK(b) value) of 7.1 for solifenacin and 7.4 for oxybutynin. To study the tissue selectivity between bladders and salivary glands, guinea pig detrusor and mouse submandibular gland cells were stimulated with CCh and monitored for intracellular Ca2+, as determined by Fura 2 fluorescence. Ca2+ mobilization of detrusor cells was inhibited equipotently by solifenacin (pK(i)=8.4) and oxybutynin (pK(i)=8.6), whereas that of the gland cells was antagonized less potently by solifenacin (pK(b)=7.4) than by oxybutynin (pK(b)=8.8), although the M-3 subtype mediated both cell responses. In anesthetized rats, solifenacin (63-2100 nmol kg(-1) or 0.03-1 mg kg(-1)) dose-dependently inhibited CCh-stimulated increases in urinary bladder pressure, while its inhibitory effects on salivation and bradycardia were apparent only at a dose of 2100 nmol kg(-1). In contrast, oxybutynin within a dose range of 77-770 nmol kg(-1) (0.03-0.3 mg kg(-1)) inhibited responses of the bladder and salivary gland slightly more potently than that of the heart. In addition, inhibitory effects of darifenacin indicated a major role Of M-3 receptors in the bladder and salivary gland. Therefore, M-3 receptor antagonism by solifenacin could be bladder-selective. This selectivity remains to be elucidated and may provide new approaches to the pharmacotherapy of overactive bladder.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 2442-10-6, in my other articles. Name: 1-Octen-3-yl Acetate.

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, SDS of cas: 140-67-0, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 140-67-0, Name is 1-Allyl-4-methoxybenzene, molecular formula is C10H12O. In an article, author is Radl, S,once mentioned of 140-67-0.

Synthesis and antinociceptive activity of some 3-chlorophenyl- and 6-chloropyridin-2-yl derivatives

Derivatives of 2-chloro-6-(4-hydroxy-1-methylpiperidin-4-yl)pyridine (2b) were prepared and tested as analgesics. 2-Chloro-6-lithiopyridine treated with quinuclidin-3-one, 1-methylpyrrolidin-3-one, 2-(dimethylaminomethyl) cyclohexanone, and ethyl 1-methylpiperidin-4-ylcarboxylate provided the corresponding alcohols 5, 6, 13a, and 6-chloro-2-pyridyl 1l-methylpiperidin-4-yl ketone (9). The ketone was reduced with sodium borohydride or treated with methylmagnesium chloride or phenyllithium to provide the corresponding alcohols 11, 12a and 12b, respectively. 1-[4-(6-Chloro-2-pyridyl)1-methyrpiperidin-4-yl]1-methylethanol (4b) was prepared from 2-chloro-6-(1-methyl-1,2,5,6-tetrahydropyridin-4-yl)pyridine (14b) by treatment with butyllithium and acetone followed by reduction of intermediate 15b with sodium cyanoborohydride.

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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. 871-91-0, Name is 7-Octyn-1-ol, molecular formula is C8H14O. In an article, author is Primozic, I,once mentioned of 871-91-0, HPLC of Formula: C8H14O.

Stereoselective hydrolysis of quaternary quinuclidinium benzoates catalyzed by butyrylcholinesterase

Four chiral, quaternary, N-methyl and N-benzyl derivatives of (R)- and (S)-quinuclidin-3-yl benzoates were synthesized and studied as substrates of horse serum butyrylcholinesterase (BChE). The k(cat) for the substrates decreased in the order (R)-N-methyl > (R)-N-benzyl (2.3-fold slower) much greater than (S)-N-methyl (70.5-fold slower reaction), while for the (S)-N-benzyl ester inhibition of the enzyme was observed. The kinetics of inhibition (K-a = 3.3 mum) indicated that binding to the catalytic site of BChE occurred. From the ratio of the k(cat)/K-M values of both enantiomers an enantiomeric excess of 95% was calculated for N-methyl derivatives. Thus, BChE is suitable as a biocatalyst for the resolution of racemic quaternary quinu-clidinium esters. In order to explain the experimental data, combined quantum chemical (HF/3-21G*) and semiempirical (PM3) calculations within the ONIOM scheme of the stable species in the acylation step were performed. Geometry optimizations were carried out for all benzoate esters for an assumed active site model of BChE. It was confirmed that hydrolysis is affected to an appreciable extent by a proper geometrical orientation of substrates at the choline subsite. The energies of the optimized systems were in good agreement with the experimental data. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).

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Electric Literature of 123-96-6, 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. 123-96-6, Name is Octan-2-ol, SMILES is CC(O)CCCCCC, belongs to quinuclidines compound. In a article, author is Brossat, Maude, introduce new discover of the category.

Simple one-pot process for the bioresolution of tertiary amino ester protic ionic liquids using subtilisin

An efficient hydrolase-catalyzed bioresolution of tertiary amino ester protic ionic liquids has been demonstrated. Protic ionic liquids have been prepared in one step from the corresponding tertiary amino alcohols by treatment with butyric anhydride. After bioresolution, unreacted esters can be easily separated from the corresponding alcohols by extraction with hexane Bioresolution of quinuclidin-3-yl butyrate has been performed with excellent selectivity. (C) 2009 Elsevier Ltd. All rights reserved.

Electric Literature of 123-96-6, 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 123-96-6 is helpful to your research.

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Related Products of 630-19-3, 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. 630-19-3, Name is Pivalaldehyde, SMILES is CC(C)(C)C=O, belongs to quinuclidines compound. In a article, author is Yildiz, Umit Hakan, introduce new discover of the category.

Real-time determination of the activity of ATPase by use of a water-soluble polythiophene

This contribution introduces a fluorescence assay for real-time determination of the activity of p97/VCP, a 540-kDa homo-hexameric enzyme, belonging to the AAA-ATPase family. A fluorescent reporter poly 1-(3-((4-methylthiophen-3-yl)oxy)propyl)quinuclidin-1-ium (poly PTQ) is used to monitor the hydrolysis of ATP to ADP by p97/VCP. The proposed assay relies on the different strength of coordination of ATP and ADP to the polymer backbone. We used recovery of fluorescence intensity on addition of p97/VCP to a poly PTQ/ATP solution to determine the enzymatic activity. The kinetic data K (m) and V (max) were 0.30 mmol L-1 ATP and 0.134 nmol ATP min(-1) mu g(-1) enzyme, respectively. The specificity of the assay was investigated by using an unhydrolyzable ATP analogue and sensitivity against p97 mutagenesis was further examined by detection of the activity of wild type and truncated p97/VCP. Our study demonstrates that determination of the real-time activity of p97/VCP is possible, because of the superior sensitivity and very fast optical response of poly PTQ.

Related Products of 630-19-3, 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 630-19-3.

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Quinuclidine – Wikipedia,
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In an article, author is Kobayashi, S, once mentioned the application of 53293-00-8, Name is 5-Hexynoic acid, molecular formula is C6H8O2, molecular weight is 112.13, MDL number is MFCD00066346, category is quinuclidines. Now introduce a scientific discovery about this category, Formula: C6H8O2.

Effects of YM905, a novel muscarinic M-3-receptor antagonist, on experimental models of bowel dysfunction in vivo

We investigated the effects of YM905 [(+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate], a new orally active muscarinic M-3-receptor antagonist, on bowel dysfunction in vivo using experimental models that reproduce the symptoms present in irritable bowel syndrome (IBS). YM905 potently inhibited restraint stress-induced fecal pellet output in fed rats (ED50: 4.0 mg/kg) and diarrhea in fasted rats (ED50: 1.7 mg/kg), with similar potencies to the inhibition of bethanechol-, neostigmine- and nicotine-induced fecal pellet output in rats (ED50: 3.3, 7.9 and 4.5 mg/kg, respectively). YM905 also inhibited 5-hydroxytryptamine (5-HT)-, prostaglandin E-2- and castor oil-induced secretory diarrhea in mice (ED50: 5.5, 14 and 6.3 mg/kg, respectively), but showed no significant effect on cholera toxin-induced intestinal secretion in mice. In addition, YM905 (3, 10 mg/kg) reversed morphine-decreased postprandial defecation in ferrets, a model of spastic constipation, whereas remosetron, a 5-HT3-receptor antagonist, was not effective. The mode of YM905 action was similar to that of darifenacin, a selective M3-receptor antagonist, with equivalent potencies. By contrast, propantheline, an antimuscarinic drug that has been used for IBS, was much less potent. These results show that YM905 ameliorates a wide spectrum of bowel dysfunctions through the blockade Of M-3 receptors, suggesting its therapeutic potential for treating IBS.

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Related Products of 2495-39-8, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 2495-39-8, Name is Sodium Allylsulfonate, SMILES is C=CCS(=O)([O-])=O.[Na+], belongs to quinuclidines compound. In a article, author is Ugawa, T, introduce new discover of the category.

YM-53601, a novel squalene synthase inhibitor, suppresses lipogenic biosynthesis and lipid secretion in rodents

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.

Related Products of 2495-39-8, 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 2495-39-8 is helpful to your research.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 22767-49-3, Name is Sodium pentane-1-sulfonate, SMILES is [Na+].CCCCCS([O-])(=O)=O, in an article , author is Venkateswaran, Amudhan, once mentioned of 22767-49-3, Computed Properties of C5H11NaO3S.

Antiangiogenic properties of substituted (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol/one analogs and their derivatives

In the past half century research efforts have defined a critical role for angiogenesis in tumor growth and metastasis. We previously reported that inhibition of a novel target, ENOX1, by a (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ol, suppressed tumor angiogenesis. The present study was undertaken in order to establish structure-activity relationships for quinuclidine analogs. The angiogenesis inhibiting activity of a series of substituted (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ols (1a-1k), (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ones (2a-2h), (Z)-(+/-)-2-(1H/N-methyl-indol-3-ylmethylene) quinuclidin-3-ols (3a-3b), and substituted (Z)-(+/-)-2-(N-benzenesulfonylindol-3-yl-methylene) quinuclidin-3-ols and their derivatives (4a-4d) that incorporate a variety of substituents in both the indole and N-benzyl moieties was evaluated using Human Umbilical Vein Endothelial Cells (HUVECs) subjected to in vitro cell migration scratch assays, tubule formation in Matrigel, cell viability and proliferation assays. In total, 25 different analogs were evaluated. Based on in vitro cell migration scratch assays, eight analogs were identified as potent angiogenesis inhibitors at 10 mu M, a concentration that was determined to be nontoxic by colony formation assay. In addition, this approach identified a potent antiangiogenic ENOX1 inhibitor, analog 4b. (C) 2010 Elsevier Ltd. All rights reserved.

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Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 112-44-7, Name is Undecanal. In a document, author is Ohtake, A, introducing its new discovery. HPLC of Formula: C11H22O.

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.

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