Day: April 20, 2021

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. 68131-04-4, Name is Sodium bicyclo[2.2.1]hept-5-ene-2,3-dicarboxylate, molecular formula is C9H8Na2O4, belongs to quinuclidines compound, is a common compound. In a patnet, author is Primozic, I, once mentioned the new application about 68131-04-4, Safety of Sodium bicyclo[2.2.1]hept-5-ene-2,3-dicarboxylate.

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.

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 68131-04-4, you can contact me at any time and look forward to more communication. Safety of Sodium bicyclo[2.2.1]hept-5-ene-2,3-dicarboxylate.

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

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¨CH bond functionalisation has revolutionised modern synthetic chemistry. 13623-94-4, Name is 1,1-Bis(methylthio)-2-nitroethylene. In a pantent, once mentioned the new application about 13623-94-4, Recommanded Product: 1,1-Bis(methylthio)-2-nitroethylene.

3-Amidoquinuclidine derivatives: Synthesis and interaction with butyrylcholinesterase

Racemates as well as (R)- and (S)-enantiomers of 3-pivalamidoquinuclidine (PivQ) and 3-acetamidoquinuclidine (AcQ) were prepared. Their quaternary racemic and enantiomerically pure N-benzyl derivatives (BnlPivQ and BnlAcQ) were synthesized as well. The amides were tested as substrates and inhibitors of butyrylcholinesterase (BChE) from horse serum (EC 3.1.1.8). No hydrolysis was observed under the experimental conditions applied. On the contrary, inhibition of BChE by (R)- and (S)-enantiomers of N-benzylquinuclidinium amides of pivalic acid was observed. The (S)-BnlPivQ with K-i = 41.57 mu mol dm(-3) was 3-fold more potent inhibitor than the (R)-enantiomer. On the other hand, preliminary results indicated that both enantiomers of N-benzylquinuclidinum amides of acetic acid may possibly be inhibitors as well as activators depending on the concentrations of benzoylcholine (BzCh) used as a substrate of BChE.

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. 13623-94-4, you can contact me at any time and look forward to more communication. Recommanded Product: 1,1-Bis(methylthio)-2-nitroethylene.

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

In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 6413-10-1, Name is Ethyl 2-(2-methyl-1,3-dioxolan-2-yl)acetate, SMILES is O=C(OCC)CC1(C)OCCO1, in an article , author is Herschorn, Sender, once mentioned of 6413-10-1, 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. 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 6413-10-1. Category: quinuclidines.

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

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.957-68-6, Name is 7-Aminocephalosporanic acid, SMILES is CC(OCC(CS[C@@]([H])(N12)[C@H](N)C2=O)=C1C(O)=O)=O, belongs to quinuclidines compound. In a document, author is Boskovic, Perica, introduce the new discover, SDS of cas: 957-68-6.

The Aggregation Behavior and Antioxidative Activity of Amphiphilic Surfactants Based on Quinuclidin-3-ol

The self-aggregation and thermodynamic properties of three cationic quaternary ammonium surfactants were investigated. The physicochemical properties of compounds containing quinuclidin-3-ol with even number of carbon atoms (10, 12, and 14) in the hydrophobic tail were measured by conductivity, dynamic light scattering (DLS), and Zeta-potential measurements. DLS and Zeta-potential measurements show a similar size distribution for all surfactants with excellent uniformity, and Zeta-potential increases significantly with increase in the size of hydrocarbon tail. The critical micelle concentration (CMC) and the degree of micelle ionization (beta) were determined using conductivity measurements. The CMC values of surfactants were found to be between 3.4 and 23.8 x 10(-3) M. The standard Gibbs free energy (Delta Gmico) was derived from conductivity measurements and suggests that surfactants containing longer chains spontaneously form micelles. The antioxidative properties of these cationic surfactants were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) assays. Among the tested samples, N-tetradecyl-3-hydroxyquinuclidinium bromide (QOH-C14) exhibited the highest antioxidative potential (388.30 nmol (TE) equivalents mL(-1)), which was further investigated by the DNA nicking assay.

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 957-68-6, you can contact me at any time and look forward to more communication. SDS of cas: 957-68-6.

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

Reference of 25265-77-4, Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter. 25265-77-4, Name is 2,2,4-Trimethyl-1,3-pentanediol 1-monoisobutyrate, SMILES is CC(C(C(C)(COC(C(C)C)=O)C)O)C.CC(C)C(OC(C(C)C)C(C)(C)CO)=O, belongs to quinuclidines compound. In a article, author is Ugawa, T, introduce new discover of the category.

YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species

1 The aim of this study was to evaluate the potency of YM-53601 ((E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a new inhibitor of squalene synthase, in reducing both plasma cholesterol and triglyceride levels, compared with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor and fibrates, respectively. 2 YM-53601 equally inhibited squalene synthase activities in hepatic microsomes prepared from several animal species and also suppressed cholesterol biosynthesis in rats (ED50, 32 mg kg(-1)). 3 In guinea-pigs, YM-53601 and pravastatin reduced plasma nonHDL-C (= total cholesterol – high density lipoprotein cholesterol) by 47% (P<0.001) and 33% (P<0.001), respectively (100 mg kg(-1), daily for 14 days). In rhesus monkeys, YM-53601 decreased plasma nonHDL-C by 37% (50 mg kg(-1) twice daily for 21 days, P<0.01), whereas the HMG-CoA reductase inhibitor, pravastatin, failed to do (25 mg kg(-1), twice daily for 28 days). 4 YM-53601 caused plasma triglyceride reduction in hamsters fed a normal diet (81% decrease at 50 mg kg-l, daily for 5 days, P<0.001). In hamsters fed a high-fat diet, the ability of YM-53601 to lower triglyceride (by 73%, P<0.001) was superior to that of fenofibrate (by 53%, P<0.001), the most potent fibrate (dosage of each drug: 100 mg kg(-1), daily for 7 days). 5 This is the first report that a squalene synthase inhibitor is superior to an HMG-CoA reductase inhibitor in lowering plasma nonHDL-C level in rhesus monkeys and is superior to a fibrate in significantly lowering plasma triglyceride level. YM-53601 may therefore prove useful in treating hypercholesterolemia and hypertriglyceridemia in humans. Reference of 25265-77-4, 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 25265-77-4 is helpful to your research.

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. 2495-37-6, Name is Benzyl methacrylate, SMILES is CC(C(OCC1=CC=CC=C1)=O)=C, belongs to quinuclidines compound. In a document, author is Visser, TJ, introduce the new discover, Recommanded Product: 2495-37-6.

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. 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 2495-37-6. Recommanded Product: 2495-37-6.

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

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. 54512-75-3, Name is 1-Bromo-5-chloropentane, molecular formula is C5H10BrCl, belongs to quinuclidines compound, is a common compound. In a patnet, author is Tudosie, Mihail S., once mentioned the new application about 54512-75-3, Computed Properties of C5H10BrCl.

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.

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 54512-75-3, you can contact me at any time and look forward to more communication. Computed Properties of C5H10BrCl.

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

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.105-50-0, Name is Diethyl 1,3-acetonedicarboxylate, SMILES is O=C(OCC)CC(CC(OCC)=O)=O, belongs to quinuclidines compound. In a document, author is Boskovic, Perica, introduce the new discover, Application In Synthesis of Diethyl 1,3-acetonedicarboxylate.

The Aggregation Behavior and Antioxidative Activity of Amphiphilic Surfactants Based on Quinuclidin-3-ol

The self-aggregation and thermodynamic properties of three cationic quaternary ammonium surfactants were investigated. The physicochemical properties of compounds containing quinuclidin-3-ol with even number of carbon atoms (10, 12, and 14) in the hydrophobic tail were measured by conductivity, dynamic light scattering (DLS), and Zeta-potential measurements. DLS and Zeta-potential measurements show a similar size distribution for all surfactants with excellent uniformity, and Zeta-potential increases significantly with increase in the size of hydrocarbon tail. The critical micelle concentration (CMC) and the degree of micelle ionization (beta) were determined using conductivity measurements. The CMC values of surfactants were found to be between 3.4 and 23.8 x 10(-3) M. The standard Gibbs free energy (Delta Gmico) was derived from conductivity measurements and suggests that surfactants containing longer chains spontaneously form micelles. The antioxidative properties of these cationic surfactants were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) assays. Among the tested samples, N-tetradecyl-3-hydroxyquinuclidinium bromide (QOH-C14) exhibited the highest antioxidative potential (388.30 nmol (TE) equivalents mL(-1)), which was further investigated by the DNA nicking assay.

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 105-50-0, you can contact me at any time and look forward to more communication. Application In Synthesis of Diethyl 1,3-acetonedicarboxylate.

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. 294-62-2, Name is Cyclododecane, SMILES is C1CCCCCCCCCCC1, belongs to quinuclidines compound. In a document, author is Madadi, Nikhil Reddy, introduce the new discover, Formula: C12H24.

Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel, high affinity ligands for CB1 and CB2 cannabinoid receptors

A small library of N-benzyl indolequinuclidinone (IQD) analogs has been identified as a novel class of cannabinoid ligands. The affinity and selectivity of these IQDs for the two established cannabinoid receptor subtypes, CB1 and CB2, was evaluated. Compounds 8 (R = R-2 = H, R-1 = F) and 13 (R = COOCH3, R-1 = R-2 = H) exhibited high affinity for CB2 receptors with K-i values of 1.33 and 2.50 nM, respectively, and had lower affinities for the CBI receptor (K-i values of 9.23 and 85.7 nM, respectively). Compound 13 had the highest selectivity of all the compounds examined, and represents a potent cannabinoid ligand with 34-times greater selectivity for CB2R over CB1R. These findings are significant for future drug development, given recent reports demonstrating beneficial use of cannabinoid ligands in a wide variety of human disease states including drug abuse, depression, schizophrenia, inflammation, chronic pain, obesity, osteoporosis and cancer. (C) 2013 Elsevier Ltd. All rights reserved.

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. 294-62-2, you can contact me at any time and look forward to more communication. Formula: C12H24.

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

In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 111-12-6, Name is Methyl oct-2-ynoate, SMILES is CCCCCC#CC(OC)=O, in an article , author is NILSSON, BM, once mentioned of 111-12-6, Quality Control of Methyl oct-2-ynoate.

3-HETEROARYL-SUBSTITUTED QUINUCLIDIN-3-OL AND QUINUCLIDIN-2-ENE DERIVATIVES AS MUSCARINIC ANTAGONISTS – SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS

A number of 3-heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives have been prepared and evaluated for muscarinic and antimuscarinic properties. The affinities of the new compounds (13, 14, 16-32, and 36-52a,b) were tested in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate [(-)-[H-3]QNB] as the radioligand and in a functional assay using isolated guinea pig urinary bladder. The present compounds behaved as competitive muscarinic antagonists in the urinary bladder. The highest receptor binding affinity, K-i (cortex) = 9.6 nM, was observed for 3-(2-benzofuranyl)quinuclidin-2-ene (31). The corresponding 3-benzofuranyl (36) and 3-benzothienyl (37) homologues had about 3.5-fold lower affinity for cortical muscarinic receptors. All quinuclidin-3-ol derivatives (14 and 16-25) had lower binding affinities for the different muscarinic receptor subtypes than the corresponding quinuclidin-2-ene analogues when examined in the various tissue homogenates. In general, the new compounds showed low subtype selectivity. The structure-affinity relationships are discussed in terms of differences in proton basicity of the azabicyclic nitrogen and differences in geometric, conformational, and/or electronic properties of the compounds. The cortical antimuscarinic potency is also related to the complementarity of the compounds to the putative binding site of the muscarinic mi receptor.

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 111-12-6. Quality Control of Methyl oct-2-ynoate.

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