Day: April 26, 2021

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.3159-07-7, Name is 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine, SMILES is C1=CC=CC2=C1C(NC3=C(S2)C=CC=C3)=O, belongs to quinuclidine compound. In a document, author is Prickaerts, Jos, introduce the new discover, Safety of 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine.

EVP-6124, a novel and selective alpha 7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of alpha 7 nicotinic acetylcholine receptors

EVP-6124, (R)-7-chloro-N-quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, is a novel partial agonist of alpha 7 neuronal nicotinic acetylcholine receptors (nAChRs) that was evaluated here in vitro and in vivo. In binding and functional experiments, EVP-6124 showed selectivity for alpha 7 nAChRs and did not activate or inhibit heteromeric alpha 4 beta 2 nAChRs. EVP-6124 had good brain penetration and an adequate exposure time. EVP-6124 (0.3 mg/kg, p.o.) significantly restored memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) in an object recognition task (ORT). Although donepezil at 0.1 mg/kg, p.o. or EVP-6124 at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory. In a natural forgetting test, an ORT with a 24 h retention time. EVP-6124 improved memory at 0.3 mg/kg, p.o. This improvement was blocked by the selective alpha 7 nAChR antagonist methyllycaconitine (0.3 mg/kg, i.p. or 10 mu g, i.c.v.). In co-application experiments of EVP-6124 with acetylcholine, sustained exposure to EVP-6124 in functional investigations in oocytes caused desensitization at concentrations greater than 3 nM, while lower concentrations (0.3-1 nM) caused an increase in the acetylcholine-evoked response. These actions were interpreted as representing a co-agonist activity of EVP-6124 with acetylcholine on alpha 7 nAChRs. The concentrations of EVP-6124 that resulted in physiological potentiation were consistent with the free drug concentrations in brain that improved memory performance in the ORT. These data suggest that the selective partial agonist EVP-6124 improves memory performance by potentiating the acetylcholine response of alpha 7 nAChRs and support new therapeutic strategies for the treatment of cognitive impairment. This article is part of a Special Issue entitled ‘Post-Traumatic Stress Disorder’. (C) 2011 Elsevier Ltd. 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 3159-07-7. Safety of 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine.

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 54512-75-3, Name is 1-Bromo-5-chloropentane, molecular formula is C5H10BrCl, molecular weight is 185.49, MDL number is MFCD00001016, category is quinuclidine. Now introduce a scientific discovery about this category, Computed Properties of C5H10BrCl.

3-LITHIOQUINUCLIDIN-2-ENE – A NOVEL INTERMEDIATE FOR THE SYNTHESIS OF MUSCARINIC AGONISTS AND ANTAGONISTS

A method for the generation of 3-lithioquinuclidin-2-ene (3) as a nucleophilic intermediate for the synthesis of 3-substituted quinuclidin-2-enes is presented.

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 54512-75-3, Computed Properties of C5H10BrCl.

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

Electric Literature of 183322-18-1, 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. 183322-18-1, Name is 4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline, SMILES is ClC1=NC=NC2=CC(=C(C=C12)OCCOC)OCCOC, belongs to quinuclidine compound. In a article, author is Chen, Li-Zhuang, introduce new discover of the category.

Quininium tetrachloridozinc(II)

The asymmetric unit of the title compound {systematic name: 2-[hydroxy(6-methoxyquinolin-1-ium-4-yl)methyl]-8-vinyl-quinuclidin-1-ium tetrachloridozinc(II)}, (C20H26N2O2)[ZnCl4], consists of a double protonated quininium cation and a tetrachloridozinc(II) anion. The Zn-II ion is in a slightly distorted tetrahedral coordination environment. The crystal structure is stabilized by intermolecular N-H center dot center dot center dot Cl and O-H center dot center dot center dot Cl hydrogen bonds.

Electric Literature of 183322-18-1, 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 183322-18-1.

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–H bond functionalisation has revolutionised modern synthetic chemistry. 25152-84-5, Name is (2E,4E)-Deca-2,4-dienal. In a pantent, once mentioned the new application about 25152-84-5, HPLC of Formula: C10H16O.

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).

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. 25152-84-5, you can contact me at any time and look forward to more communication. HPLC of Formula: C10H16O.

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 Primozic, Ines, once mentioned the application of 2179-57-9, Name is Diallyldisulfide, molecular formula is C6H10S2, molecular weight is 146.2736, MDL number is MFCD00008656, category is quinuclidine. Now introduce a scientific discovery about this category, Recommanded Product: Diallyldisulfide.

Binding Modes of Quinuclidinium Esters to Butyrylcholinesterase

The orientations of chiral quinuclidin-3-ol esters and benzoylcholine in the active site of horse butyrylcholinesterase have been investigated by flexible ligand docking. Change of the esters’ acyl moiety as well as the substituent at the quinuclidinium nitrogen atom affected the activity and stereoselectivity of the biotransformations. Analysis of interactions in the active site revealed the most important binding patterns for enantiomers, which define their reactivity. Calculated Gibbs energies of binding obtained by molecular docking simulations were well correlated to the experimentally determined binding affinities of the investigated chiral esters. (doi: 10.5562/cca2060)

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 2179-57-9, you can contact me at any time and look forward to more communication. Recommanded Product: Diallyldisulfide.

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–H bond functionalisation has revolutionised modern synthetic chemistry. 2386-53-0, Name is Sodium dodecane-1-sulfonate. In a pantent, once mentioned the new application about 2386-53-0, Safety of Sodium dodecane-1-sulfonate.

Enantiomers of quinuclidin-3-ol derivatives: Resolution and interactions with human cholinesterases

The (R)- and (S)-enantiomers of quinuclidin-3-ol and quinuclidin-3-yl acetate as well as their quaternary N-methyl and N-benzyl derivatives were synthesized in order to study the stereo-selectivity of human erythrocyte acetylcholinesterase (EC 3.1.1.7) and plasma butyrylcholinesterase (EC 3.1.1.8). The compounds were tested as substrates and inhibitors of cholinesterases. Both cholinesterases hydrolyze the derivatives of quinuclidin-3-yl acetate with a preference for the (R)- over (S)-enantiomers. In contrast to the hydrolysis of the enantiomers of acetates, the inhibition of acetylcholinesterase and butyrylcholinesterase by the (R)- and (S)-enantiomers of quinuclidin-3-ol derivatives does not reveal enantiomeric preference of the enzymes. The (R)and (S)-acetates also act as nonstereoselective inhibitors of the enzyme-induced hydrolysis of acetylthiocholine. The best substrate is (R)-N-methyl-3-acetoxyquinuclidinium iodide with k(cat) = 1.5 x 10(6) min(-1) and k(cat) = 5.5 x 10(4) min(-1) for acetylcholinesterase and butyrylcholinesterase, respectively. The (R)- and (S)-N-benzylquinuclidinium derivatives are the most potent inhibitors of both enzymes.

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 2386-53-0. The above is the message from the blog manager. Safety of Sodium dodecane-1-sulfonate.

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

Electric Literature of 5390-04-5, 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. 5390-04-5, Name is 4-Pentyn-1-ol, SMILES is C#CCCCO, belongs to quinuclidine compound. In a article, author is Ohtake, A, introduce new discover of the category.

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.

Electric Literature of 5390-04-5, 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 5390-04-5 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. 112-59-4, Name is 2-(2-(Hexyloxy)ethoxy)ethanol, SMILES is OCCOCCOCCCCCC, belongs to quinuclidine compound. In a document, author is Primozic, Ines, introduce the new discover, Product Details of 112-59-4.

Preparation of Novel meta- and para-Substituted N-Benzyl Protected Quinuclidine Esters and Their Resolution with Butyrylcholinesterase

Since the optically active quinuclidin-3-ol is an important intermediate in the preparation of physiologically or pharmacologically active compounds, a new biocatalytic method for the production of chiral quinuclidin-3-ols was examined. Butyrylcholinesterase (BChE; EC 3.1.1.8) was chosen as a biocatalyst in a preparative kinetic resolution of enantiomers. A series of racemic, (R)- and (S)-esters of quinuclidin-3-ol and acetic, benzoic, phthalic and isonicotinic acids were synthesized, as well as their racemic quaternary N-benzyl, meta- and para-N-bromo and N-methylbenzyl derivatives. After the resolution, all N-benzyl protected groups were successfully removed by catalytic transfer hydrogenation with ammonium formate (10% Pd-C). Hydrolyses studies with BChE confirmed that (R)-enantiomers of the prepared esters are much better substrates for the enzyme than (S)-enantiomers. Introduction of bromine atom or methyl group in the meta or para position of the benzyl moiety resulted in a considerable improvement of the stereoselectivity compared to the non-substituted compounds. Optically pure quinuclidin-3-ols were prepared in high yields and enantiopurity by the usage of various N-benzyl protected groups and BChE as a biocatalyst.

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 112-59-4. The above is the message from the blog manager. Product Details of 112-59-4.

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 C15H14N2O, 3564-73-6, Name is 10,11-Dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, SMILES is O=C(N1C2=CC=CC=C2CCC3=CC=CC=C31)N, in an article , author is Klimova, EI, once mentioned of 3564-73-6.

Stereospecific formation of polycyclic ferrocenyldihydropyrazoles based on Z- and E-isomeric ferrocenyl- substituted alpha,beta-unsaturated ketones of the heterocyclic series

The reactions of E- and Z-isomeric 2-(ferrocenylmethylidene)quinuclidin-3-one, 1-methyl-3-(ferrocenylmethylidene)piperidin-4-one, and 2-(ferrocenylmethylidene)tropinone with hydrazine proceed stereospecifically to form the same diastereomeric polycyclic ferrocenyldihydropyrazoles regardless of the geometrical configuration of the starting alpha,beta -unsaturated ketones. The structure of the trans-diastereomer of 4-acetyl-3-ferrocenyl-1,4,5-triazatricyclo[5.2.2.0(2,6)]undec-5-ene was established by X-ray diffraction analysis.

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 3564-73-6. The above is the message from the blog manager. Computed Properties of C15H14N2O.

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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. 2495-39-8, Name is Sodium Allylsulfonate, SMILES is C=CCS(=O)([O-])=O.[Na+], in an article , author is CLARK, RD, once mentioned of 2495-39-8, Safety of Sodium Allylsulfonate.

N-(QUINUCLIDIN-3-YL)-2-(1-METHYL-1H-INDOL-3-YL)-2-OXOACETAMIDE – A HIGH-AFFINITY 5-HT3 RECEPTOR PARTIAL AGONIST

The enantiomers of the indolyl-2-oxoacetamide 5 were found to have 5-HT3 receptor partial agonist activity with(R)-5 having higher potency than (S)-5.

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 2495-39-8. The above is the message from the blog manager. Safety of Sodium Allylsulfonate.

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