Day: March 25, 2021

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 25952-53-8, Name is 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, molecular formula is C8H18ClN3, belongs to quinuclidines compound, is a common compound. In a patnet, author is Ikeda, K, once mentioned the new application about 25952-53-8, Application In Synthesis of 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride.

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.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 25952-53-8. The above is the message from the blog manager. Application In Synthesis of 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride.

Reference:
Quinuclidine – Wikipedia,
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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. 112-59-4, Name is 2-(2-(Hexyloxy)ethoxy)ethanol, molecular formula is C10H22O3. In an article, author is Shchekotikhin, AE,once mentioned of 112-59-4, Formula: C10H22O3.

3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione for circumvention of anticancer drug resistance

A series of 3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3 -f]indole-5,10-dione was synthesized by Mannich reaction or by the transamination of 3-dimethylaminomethyl 4,11-dihydroxy- or 4,11-dimethoxynaphtho[2,3-f]indole-5,10-dione. The potency of novel derivatives was tested on a National Cancer Institute panel of 60 human tumor cell lines as well as in cells with genetically defined determinants of cytotoxic drug resistance, P-glycoprotein (Pgp) expression, and p53 inactivation. Mannich derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione with an additional amino function in their side chain, demonstrated equal cytotoxicity against the parental K562 leukemia cells and their Pgp-positive subline, whereas the latter showed similar to 7-fold resistance to adriamycin, a Pgp transported drug. 3-(1-Piperazinyl)methyl and 3-(quinuclidin-3-yl)aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione killed HCT116 colon carcinoma cells (carrying wild type p53) and their p53-null variant within the similar range of concentrations. We conclude that Mannich modification of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione, especially when cyclic diamine (e.g., piperazine, quinuclidine) is used, confers an important feature to the resulting compounds, namely, the potency for tumor cells otherwise resistant to a variety of anticancer drugs. (c) 2004 Elsevier Ltd. All rights reserved.

Interested yet? Keep reading other articles of 112-59-4, you can contact me at any time and look forward to more communication. Formula: C10H22O3.

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Quinuclidine – Wikipedia,
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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, Formula: C6H10O, 6728-26-3, Name is trans-2-Hexenal, SMILES is CCC/C=C/C=O, belongs to quinuclidines compound. In a document, author is Suzuki, M, introduce the new discover.

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.

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 6728-26-3 is helpful to your research. Formula: C6H10O.

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

Electric Literature of 112-59-4, 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. 112-59-4, Name is 2-(2-(Hexyloxy)ethoxy)ethanol, SMILES is OCCOCCOCCCCCC, belongs to quinuclidines compound. In a article, author is Tang, Cuyue, introduce new discover of the category.

Neuropharmacokinetics of two investigational compounds in rats: Divergent temporal profiles in the brain and cerebrospinal fluid

Two investigational compounds (FRM-1, (R)-7-fluoro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and FRM-2, (R)-7-cyano-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide) resided in rat brain longer than in systemic circulation. In Caco-2 directional transport studies, they both showed good intrinsic passive permeability but differed significantly in efflux susceptibility (efflux ratio of <2 and similar to 7, respectively), largely attributed to P-glycoprotein (P-gp). Capitalizing on these interesting properties, we investigated how cerebrospinal fluid (CSF) concentration (C-CSF) would be shaped by unbound plasma concentration (C-u,C-p) and unbound brain concentration (C-u,C-b) in disequilibrium conditions and at steady state. Following subcutaneous administration, FRM-1 C-CSF largely followed C-u,C-p initially and leveled between C-u,C-p and C-u,C-b. However, it gradually approached C-u,C-b and became lower than, but parallel to C-u,C-b at the terminal phase. In contrast, FRM-2 C-CSF temporal profile mostly paralleled the C-u,C-p but was at a much lower level. Upon intravenous infusion to steady state, FRM-1 C-CSF and C-u,C-b were similar, accounting for 61% and 69% of the Cu, indicating a case of largely passive diffusion-governed brain penetration where C-CSF served as a good surrogate for C-u,C-b. On the contrary, FRM-2 C-CSF and C-u,C-b were remarkably lower than C-u,C-p, (17% and 8% of C-u,C-p respectively), suggesting that FRM-2 brain penetration was severely impaired by P-gp-mediated efflux and C-CSF underestimated this impact. A semi-physiologically based pharmacokinetic (PBPK) model was constructed that adequately described the temporal profiles of the compounds in the plasma, brain and CSF. Our work provided some insight into the relative importance of blood-brain barrier (BBB) and blood-CSF barrier (BCSFB) in modulating CCSF. (C) 2014 Elsevier Inc. All rights reserved. Electric Literature of 112-59-4, 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. you can also check out more blogs about 112-59-4.

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

Related Products of 5781-53-3, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 5781-53-3, Name is Methyl 2-chloro-2-oxoacetate, SMILES is O=C(OC)C(Cl)=O, 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.

Related Products of 5781-53-3, 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. you can also check out more blogs about 5781-53-3.

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Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 111-87-5, Name is n-Octanol, molecular formula is C8H18O. In an article, author is Nordvall, G,once mentioned of 111-87-5, Recommanded Product: n-Octanol.

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.

Interested yet? Keep reading other articles of 111-87-5, you can contact me at any time and look forward to more communication. Recommanded Product: n-Octanol.

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Quinuclidine – Wikipedia,
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111-87-5, Name is n-Octanol, molecular formula is C8H18O, belongs to quinuclidines compound, is a common compound. In a patnet, author is Ishihara, T, once mentioned the new application about 111-87-5, Category: quinuclidines.

Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: Enzyme inhibition and effects on plasma lipid levels

Squalene synthase (E.C. 2.5.1.21) is a microsomal enzyme which catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene, and is involved in the first committed step in cholesterol biosynthesis. It is an attractive target for hypocholesterolemic and hypotriglyceridemic strategies. We synthesized a series of 3-ethylidenequinuclidine derivatives, and evaluated their ability to inhibit squalene synthase in vitro and to lower non-HDL cholesterol levels in hamsters. 3-Ethylidene-quinuclidine derivatives incorporating an unsubstituted 9H-carbazole moiety reduced plasma non-HDL cholesterol levels and did not affect plasma transaminase levels, indicating a lack of hepatotoxicity. Among the novel Compounds, (Z)-2-[2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 8 (YM-53579) and (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 28 (YM-53601) were potent inhibitors of squalene synthase derived from human hepatoma cells, with IC50 Values Of 160 and 79 nM. respectively. They also reduced plasma non-HDL cholesterol levels in hamsters by approximately 50 and 70%, respectively. at all oral dose of 50 mg/kg/day for 5 days. (C) 2003 Elsevier Ltd. All rights reserved.

If you¡¯re interested in learning more about 111-87-5. The above is the message from the blog manager. Category: quinuclidines.

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Quinuclidine – Wikipedia,
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Let¡¯s face it, organic chemistry can seem difficult to learn, Recommanded Product: Ethyl 2-oxocyclopentanecarboxylate, Especially from a beginner¡¯s point of view. Like 611-10-9, Name is Ethyl 2-oxocyclopentanecarboxylate, molecular formula is quinuclidines, belongs to quinuclidines compound. In a document, author is Ugawa, T, introducing its new discovery.

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. If you are hungry for even more, make sure to check my other article about 611-10-9, Recommanded Product: Ethyl 2-oxocyclopentanecarboxylate.

Reference:
Quinuclidine – Wikipedia,
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Related Products of 502-49-8, 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. 502-49-8, Name is Cyclooctanone, SMILES is O=C1CCCCCCC1, belongs to quinuclidines compound. In a article, author is Prickaerts, Jos, introduce new discover of the category.

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.

Related Products of 502-49-8, 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 502-49-8.

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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. 143-08-8, Name is Nonan-1-ol, molecular formula is C9H20O. In an article, author is Lima, Fabio,once mentioned of 143-08-8, Quality Control of Nonan-1-ol.

A Lewis Base Catalysis Approach for the Photoredox Activation of Boronic Acids and Esters

We report herein the use of a dual catalytic system comprising a Lewis base catalyst such as quinuclidin-3-ol or 4-dimethylaminopyridine and a photoredox catalyst to generate carbon radicals from either boronic acids or esters. This system enabled a wide range of alkyl boronic esters and aryl or alkyl boronic acids to react with electron-deficient olefins via radical addition to efficiently form C-C coupled products in a redox-neutral fashion. The Lewis base catalyst was shown to form a redox-active complex with either the boronic esters or the trimeric form of the boronic acids (boroxines) in solution.

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Quinuclidine – Wikipedia,
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