Day: March 26, 2021

Electric Literature of 583-60-8, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 583-60-8, Name is 2-Methylcyclohexanone, SMILES is O=C1C(C)CCCC1, belongs to quinuclidines compound. In a article, author is Del Bello, Fabio, introduce new discover of the category.

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments

To obtain novel muscarinic acetylcholine receptor (mAChR) antagonists, the enantiomers of the hybrid compounds 3-5, in which the quinuclidin-3-yloxy fragment of solifenacin and the 6,6-diphenyl-1,4dioxane-2-yl moiety of 2 linked by an ester or ether spacer were embedded in the same chemical entity, were prepared and evaluated for their affinity at the five mAChR subtypes (M-1-M-5). Stereochemistry and the nature of the linker between the quinuclidine moiety and the 1,4-dioxane nucleus play an important role on the affinities of the compounds. The presence of an ether bridge confers higher affinities for all mAChR subtypes to the ligand. Interestingly, the ether enantiomer (R,S)-5 shows the highest affinity at all mAChR subtypes with K-p(i) values similar to that of solifenacin at M-3 and higher at the other subtypes. Unlike solifenacin, it shows a preference for M-1 mAChR subtype with respect to the other subtypes. This compound, lacking a permanent positive charge on the nitrogen atom, can be a useful tool for the pharmacological study of mAChRs in the central nervous system. (C) 2017 Elsevier Masson SAS. All rights reserved.

Electric Literature of 583-60-8, 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 583-60-8 is helpful to your research.

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

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Safety of Oxalic acid dihydrate, 6153-56-6, Name is Oxalic acid dihydrate, SMILES is O=C(O)C(O)=O.[H]O[H].[H]O[H], belongs to quinuclidines compound. In a document, author is Ugawa, T, introduce the new discover.

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.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 6153-56-6 is helpful to your research. Safety of Oxalic acid dihydrate.

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

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Name: (E)-4-methoxy-4-oxobut-2-enoic acid, 2756-87-8, Name is (E)-4-methoxy-4-oxobut-2-enoic acid, SMILES is O=C(O)/C=C/C(OC)=O, belongs to quinuclidines compound. In a document, author is Naito, Ryo, introduce the new discover.

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.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 2756-87-8. Name: (E)-4-methoxy-4-oxobut-2-enoic acid.

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

Application of 4771-80-6, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 4771-80-6, Name is Cyclohex-3-enecarboxylic acid, SMILES is OC(=O)C1CCC=CC1, belongs to quinuclidines compound. In a article, author is Suzuki, M, introduce new discover of the category.

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.

Application of 4771-80-6, 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 4771-80-6.

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

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. 924-50-5, Name is Methyl-3,3-dimethylacrylate, molecular formula is C6H10O2. In an article, author is Klimova, EI,once mentioned of 924-50-5, Application In Synthesis of Methyl-3,3-dimethylacrylate.

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.

Interested yet? Keep reading other articles of 924-50-5, you can contact me at any time and look forward to more communication. Application In Synthesis of Methyl-3,3-dimethylacrylate.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 4070-80-8, Name is Sodium 2-octadecylfumarate, SMILES is O=C(OCCCCCCCCCCCCCCCCCC)/C=C/C([O-])=O.[Na+], belongs to quinuclidines compound. In a document, author is Del Bello, Fabio, introduce the new discover, Recommanded Product: 4070-80-8.

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments

To obtain novel muscarinic acetylcholine receptor (mAChR) antagonists, the enantiomers of the hybrid compounds 3-5, in which the quinuclidin-3-yloxy fragment of solifenacin and the 6,6-diphenyl-1,4dioxane-2-yl moiety of 2 linked by an ester or ether spacer were embedded in the same chemical entity, were prepared and evaluated for their affinity at the five mAChR subtypes (M-1-M-5). Stereochemistry and the nature of the linker between the quinuclidine moiety and the 1,4-dioxane nucleus play an important role on the affinities of the compounds. The presence of an ether bridge confers higher affinities for all mAChR subtypes to the ligand. Interestingly, the ether enantiomer (R,S)-5 shows the highest affinity at all mAChR subtypes with K-p(i) values similar to that of solifenacin at M-3 and higher at the other subtypes. Unlike solifenacin, it shows a preference for M-1 mAChR subtype with respect to the other subtypes. This compound, lacking a permanent positive charge on the nitrogen atom, can be a useful tool for the pharmacological study of mAChRs in the central nervous system. (C) 2017 Elsevier Masson SAS. All rights reserved.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 4070-80-8 is helpful to your research. Recommanded Product: 4070-80-8.

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

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 140-67-0, Name is 1-Allyl-4-methoxybenzene. In a document, author is Lee, Na-Ra, introducing its new discovery. Computed Properties of C10H12O.

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.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 140-67-0 help many people in the next few years. Computed Properties of C10H12O.

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

Related Products of 2756-87-8, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 2756-87-8, Name is (E)-4-methoxy-4-oxobut-2-enoic acid, SMILES is O=C(O)/C=C/C(OC)=O, belongs to quinuclidines compound. In a article, author is Primozic, I, introduce new discover of the category.

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).

Related Products of 2756-87-8, 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 2756-87-8.

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

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. 1490-25-1, Name is Methyl 4-chloro-4-oxobutanoate, molecular formula is , belongs to quinuclidines compound. In a document, author is Macor, JE, Safety of Methyl 4-chloro-4-oxobutanoate.

A chiral synthesis of (-)-spiro[1-azabicyclo[2.2.2] octane-3,5 ‘-oxazolidin-2 ‘-one]: A conformationally restricted analogue of acetylcholine that is a potent and selective alpha 7 nicotinic receptor agonist

A direct, short chiral synthesis of the selective 0 nicotinic receptor agonist (-)-spiro[l-azabicyclo[2.2.2]octane-3,5′-oxazolidin-2’-one] (AR-R17779) is presented. The key step utilized attack of the dianion of the (R)-HYTRA ester [(R)-(+)-2-hydroxy-1,2,2-triphenylethyl acetate] on quinuclidin-3-one, followed by a selective precipitation of the diasteriomeric tertiary alcohol that led to (S)-(-)-AR-R17779 in two additional steps.

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 1490-25-1, in my other articles. Safety of Methyl 4-chloro-4-oxobutanoate.

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

Electric Literature of 611-10-9, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 611-10-9, Name is Ethyl 2-oxocyclopentanecarboxylate, SMILES is C(OC(C1C(CCC1)=O)=O)C, belongs to quinuclidines compound. In a article, author is d’Agostino, Simone, introduce new discover of the category.

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.

Electric Literature of 611-10-9, 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 611-10-9 is helpful to your research.

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