Month: May 2021

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 54512-75-3, Name is 1-Bromo-5-chloropentane. In a document, author is Ugawa, T, introducing its new discovery. COA of Formula: https://www.ambeed.com/products/54512-75-3.html.

Experimental model of escape phenomenon in hamsters and the effectiveness of YM-53601 in the model

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. 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 54512-75-3. COA of Formula: https://www.ambeed.com/products/54512-75-3.html.

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

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. 535-75-1, Name is Pipecolinic Acid, SMILES is O=C(C1NCCCC1)O, in an article , author is Primozic, I, once mentioned of 535-75-1, Formula: https://www.ambeed.com/products/535-75-1.html.

Structural basis for selectivity of butyrylcholinesterase towards enantiomeric quinuclidin-3-yl benzoates: a quantum chemical study

In order to explain different rates of hydrolysis of (R)- and (S)-quinuclidin-3-yl benzoates and benzoylcholine catalyzed with butyrylcholinesterase, semiempirical PM3 calculations were performed with an assumed active site model of human BChE (20 amino acids). Contributions of different protein residues to the stabilization of Michaelis complexes and tetrahedral intermediates were analyzed. It was shown that the hydrolysis rates of quinuclidinium enantiomers were to an appreciable extent affected by the existence or absence of the hydrogen bond between the quinuclidinium N+-H group and the protein residues. Calculations indicated that the better stabilization of quinuclidinium moiety in the Michaelis complex than in the tetrahedral intermediate was the main reason for a greater barrier and a slower reaction rate of the (R)-enantiomer of quinuclidinium esters compared to benzoylcholine. In the case of (S)-enantiomer, the calculation indicated that the barrier to the substrate reorientation from a favourable, but non-productive binding to a productive one significantly influenced the rate of hydrolysis.

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 535-75-1, you can contact me at any time and look forward to more communication. Formula: https://www.ambeed.com/products/535-75-1.html.

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

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. 112-43-6, Name is 10-Undecen-1-ol, SMILES is C=CCCCCCCCCCO, belongs to quinuclidine compound. In a document, author is Lee, Na-Ra, introduce the new discover, COA of Formula: https://www.ambeed.com/products/112-43-6.html.

Muscarinic agonist, ( +/- )-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl) carbamate: High affinity, but low subtype selectivity for human M-1 – M-5 muscarinic acetylcholine receptors

Novel quinuclidinyl N-phenylcarbamate analogs were synthesized, and binding affinities at M-1-M-5 muscarinic acetylcholine receptor (mAChR) subtypes were determined using Chinese hamster ovary (CHO) cell membranes stably expressing one specific subtype of human mAChR. Although not subtype selective, the lead analog ( +/- )-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate (3c) exhibited the highest affinity (K-i = 2.0, 13, 2.6, 2.2, 1.8 nM) at each of the M-1-M-5 mAChRs, respectively. Based on results from the [H-3]dopamine release assay using rat striatal slices, 3c acted as an agonist at mAChRs. The effect of 3c was inhibited by the nonselective mAChR antagonist, scopolamine, and 3c augmented release evoked by oxotremorine. A potent analog from the same scaffold, ( +/- )-quinuclidin-3-yl-(4-methoxyphenethyl)(phenyl)-carbamate (3b) exhibited the greatest selectivity (17-fold) at M-3 over M-2 mAChRs. These analogs could serve as leads for further discovery of novel subtype-selective muscarinic ligands with the goal of providing therapeutics for substance use disorders and chronic obstructive pulmonary disease.

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 112-43-6. COA of Formula: https://www.ambeed.com/products/112-43-6.html.

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

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 5405-41-4, Name is Ethyl 3-hydroxybutanoate. In a document, author is d’Agostino, Simone, introducing its new discovery. COA of Formula: https://www.ambeed.com/products/5405-41-4.html.

Intriguing Case of Pseudo-Isomorphism between Chiral and Racemic Crystals of rac- and (S)/(R)2-(1,8-Naphthalimido)-2-quinuclidin-3-yl, and Their Reactivity Toward I-2 and 1Br

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.

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 5405-41-4. COA of Formula: https://www.ambeed.com/products/5405-41-4.html.

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

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 112-86-7, Name is (Z)-Docos-13-enoic acid. In a document, author is Suzuki, M, introducing its new discovery. Category: quinuclidines.

Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarcted rats

Solifenacin succinate [YM905, (+)-(1S,3′ R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] is a novel muscarinic receptor antagonist. We examined the effects of solifenacin and two other muscarinic receptor antagonists, tolterodine and propiverine, on detrusor overactivity in cerebral infarcted rats. Evaluation was done under conscious conditions using cystometry 1 day after middle cerebral artery occlusion. The cerebral infarcted rats showed decreases in bladder capacity and voided volume and an increase in residual volume, but no change in micturition pressure. Solifenacin increased bladder capacity and voided volume at doses of 0.03 mg/kg i.v. or more. Tolterodine increased bladder capacity and voided volume at 0.03 and 0.1 mg/kg i.v., while propiverine increased bladder capacity and voided volume at 1 mg/kg i.v. and at 0.3 and 1 mg/kg i.v., respectively. In contrast, none of the three drugs affected residual volume or micturition pressure. These results suggest that solifenacin may improve detrusor overactivity without causing urinary retention and may be a promising drug in the treatment of patients with overactive bladder syndrome. (c) 2005 Elsevier B.V. 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 112-86-7, Category: quinuclidines.

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

Electric Literature of 6413-10-1, Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. 6413-10-1, Name is Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate, SMILES is O=C(OCC)CC1(C)OCCO1, belongs to quinuclidine compound. In a article, author is Naito, R, introduce new discover of the category.

Selective muscarinic antagonists. II. Synthesis and antimuscarinic properties of biphenylylcarbamate derivatives

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.

Electric Literature 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,
,Quinuclidine | C7H13N | ChemSpider

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. Computed Properties of https://www.ambeed.com/products/123-96-6.html, 123-96-6, Name is Octan-2-ol, SMILES is CC(O)CCCCCC, in an article , author is Liu, Yu-Min, once mentioned of 123-96-6.

Stereoselective synthesis of the optical isomers of a new muscarinic receptor antagonist, quinuclidin-3-yl 2-(cyclopent-1-enyl)-2-hydroxy2-phenylacetate

The enantiopure isomers of a new muscarinic receptor antagonist, quinuclidin-3-yl 2-(cyclopent-1-enyl)-2-hydroxy-2-phenylacetate were synthesised by a practical stereoselective synthetic method, using pivaldehyde as steric hindrance agent from the chiral starting material, (S) or (R)-mandelic acid. The isomers were obtained with 72-78% yields in 98-99% e.e.

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 123-96-6, Computed Properties of https://www.ambeed.com/products/123-96-6.html.

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

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 Nordvall, G, once mentioned the application of 5392-40-5, Name is 3,7-Dimethylocta-2,6-dienal, molecular formula is C10H16O, molecular weight is 152.2334, MDL number is MFCD00006997, category is quinuclidine. Now introduce a scientific discovery about this category, Application In Synthesis of 3,7-Dimethylocta-2,6-dienal.

3-(2-benzofuranyl)quinuclidin-2-ene derivatives: Novel muscarinic antagonists

A series of 26 derivatives of the novel muscarinic antagonist 3-(2-benzofuranyl) quinuclidin-2-ene (1) has been synthesized and evaluated for muscarinic and antimuscarinic properties. The affinity of the compounds was determined by competition experiments in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate as the radioligand, and the antimuscarinic potency was determined in a functional assay on isolated guinea pig urinary bladder using carbachol as the agonist. The 5-fluorobenzofuranyl derivative was slightly more potent than 1. The 7-bromo-substituted 8 displayed a 14-fold tissue selectivity ratio for muscarinic receptors in the cortex versus the parotid gland. Comparative molecular field analysis and quantitative structure-activity relationship models were developed for this series of substituted benzofuranyl derivatives.

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 5392-40-5, you can contact me at any time and look forward to more communication. Application In Synthesis of 3,7-Dimethylocta-2,6-dienal.

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

Reference of 765-70-8, Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. 765-70-8, Name is 3-Methylcyclopentane-1,2-dione, SMILES is O=C1C(C(C)CC1)=O, belongs to quinuclidine compound. In a article, author is Odzak, R, introduce new discover of the category.

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.

Reference of 765-70-8, 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 765-70-8.

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

Application of 112-92-5, 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. 112-92-5, Name is 1-Hydroxyoctadecane, SMILES is CCCCCCCCCCCCCCCCCCO, belongs to quinuclidine compound. In a article, author is Nagashima, Shinya, introduce new discover of the category.

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action in a rat model than tiotropium bromide. (C) 2014 Elsevier Ltd. All rights reserved.

Application of 112-92-5, 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 112-92-5.

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