Category: quinuclidines

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,
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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.

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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, 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.

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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 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.

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Quinuclidine – Wikipedia,
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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, 1490-25-1, Name is Methyl 4-chloro-4-oxobutanoate, SMILES is O=C(OC)CCC(Cl)=O, in an article , author is Huang, Mei, once mentioned of 1490-25-1, Category: quinuclidines.

The novel alpha 7 nicotinic acetylcholine receptor agonist EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens

Background Alpha7 and alpha 4 beta 2 nicotinic acetylcholine receptor (nAChR) agonists have been shown to improve cognition in various animal models of cognitive impairment and are of interest as treatments for schizophrenia, Alzheimer’s disease, and other cognitive disorders. Increased release of dopamine (DA), acetylcholine (ACh), glutamate (Glu), and gamma-aminobutyric acid (GABA) in cerebral cortex, hippocampus, and nucleus accumbens (NAC) has been suggested to contribute to their beneficial effects on cognition. Results Using in vivo microdialysis, we found that EVP-6124 [(R)-7-chloro-N-quinuclidin-3-yl) benzo[b] thiophene-2-carboxamide], a high-affinity alpha 7 nAChR partial agonist, at 0.1 mg/kg, s.c., increased DA efflux in the medial prefrontal cortex (mPFC) and NAC. EVP-6124, 0.1 and 0.3 mg/kg, also increased efflux of ACh in the mPFC but not in the NAC. Similarly, EVP-6124, 0.1 mg/kg, but not 0.03 and 0.3 mg/kg, significantly increased mPFC Glu efflux. Thus, EVP-6124 produced an inverted U-shaped curve for DA and Glu release, as previously reported for other alpha 7 nAChR agonists. The three doses of EVP-6124 did not produce a significant effect on GABA efflux in either region. Pretreatment with the selective alpha 7 nAChR antagonist, methyllycaconitine (MLA, 1.0 mg/kg), significantly blocked cortical DA and Glu efflux induced by EVP-6124 (0.1 mg/kg), suggesting that the effects of EVP-6124 on these neurotransmitters were due to alpha 7 nAChR agonism. MLA only partially blocked the effects of EVP-6124 on ACh efflux in the mPFC. Conclusion These results suggest increased cortical DA, ACh, and Glu release, which may contribute to the ability of the alpha 7 nAChR agonist, EVP-6124, to treat cognitive impairment and possibly other dimensions of psychopathology.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 1490-25-1, you can contact me at any time and look forward to more communication. Category: quinuclidines.

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Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Related Products of 2442-10-6, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 2442-10-6, Name is 1-Octen-3-yl Acetate, SMILES is CC(OC(CCCCC)C=C)=O, belongs to quinuclidines compound. In a article, author is Nomoto, F, introduce new discover of the category.

A practical chemoenzymatic process to access (R)-quinuclidin-3-ol on scale

(+/-)-3-Butyryloxyquinuclidinium butyrate 6 (2 M, 571 g/L), prepared from (+/-)-quinuclidin-3-ol 1 and butyric anhydride, undergoes enantioselective hydrolysis by an Aspergillus melleus protease {1.0% (w/v)} in water in the presence of Ca(OH)(2) to keep the reaction at pH 7 and trap butyric acid that is introduced as part of (+/-)-6 and generated by the enzymatic hydrolysis. After a 24 h period, extraction with n-heptane provides (R)-quinuclidin-3-yl butyrate 5a, which, on methanolysis with Na2CO3, is converted into (R)-1, a common pharmacophore of neuromodulators acting on muscarinic receptors, in 96% ee and 42% overall yield from (+/-)-1. The unwanted antipode (S)-1, which is extracted into n-butanol and purified via its hydrochloride salt in 89% ee and 40% overall yield from (+/-)-1, can be racemized by the catalysis of Raney Co at 140degreesC under an atmosphere of H, (5 kg/cm(2)) to regenerate (+/-)-1 in 97% yield. (C) 2003 Elsevier Science Ltd. All rights reserved.

Related Products of 2442-10-6, 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 2442-10-6.

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Quinuclidine – Wikipedia,
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Reference of 5324-84-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 5324-84-5, Name is Sodium octane-1-sulfonate, SMILES is CCCCCCCCS(=O)([O-])=O.[Na+], belongs to quinuclidines compound. In a article, author is Penthala, Narsimha Reddy, introduce new discover of the category.

(2Z,3E)-2-{[1-(4-Chlorobenzyl)-1H-indol-3-yl]methylidene}quinuclidin-3-one oxime

In the title compound, C23H22ClN3O, the benzene ring of the 4-chorobenzyl group makes a dihedral angle of 78.56 (6)degrees with the best plane of the indole ring. The double bond connecting the azabicyclic and indole groups adopts a Z geometry. The geometry adopted by the C=N bond with respect to the N-OH bond is trans. The absolute configuration of the compound was determined from refinement of the Flack parameter.

Reference of 5324-84-5, 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 5324-84-5 is helpful to your research.

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Quinuclidine – Wikipedia,
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Synthetic Route of 97-65-4, 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. 97-65-4, Name is Propylenedicarboxylic acid, SMILES is O=C(O)C(CC(O)=O)=C, belongs to quinuclidines compound. In a article, author is Nomoto, F, introduce new discover of the category.

A practical chemoenzymatic process to access (R)-quinuclidin-3-ol on scale

(+/-)-3-Butyryloxyquinuclidinium butyrate 6 (2 M, 571 g/L), prepared from (+/-)-quinuclidin-3-ol 1 and butyric anhydride, undergoes enantioselective hydrolysis by an Aspergillus melleus protease {1.0% (w/v)} in water in the presence of Ca(OH)(2) to keep the reaction at pH 7 and trap butyric acid that is introduced as part of (+/-)-6 and generated by the enzymatic hydrolysis. After a 24 h period, extraction with n-heptane provides (R)-quinuclidin-3-yl butyrate 5a, which, on methanolysis with Na2CO3, is converted into (R)-1, a common pharmacophore of neuromodulators acting on muscarinic receptors, in 96% ee and 42% overall yield from (+/-)-1. The unwanted antipode (S)-1, which is extracted into n-butanol and purified via its hydrochloride salt in 89% ee and 40% overall yield from (+/-)-1, can be racemized by the catalysis of Raney Co at 140degreesC under an atmosphere of H, (5 kg/cm(2)) to regenerate (+/-)-1 in 97% yield. (C) 2003 Elsevier Science Ltd. All rights reserved.

Synthetic Route of 97-65-4, 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 97-65-4 is helpful to your research.

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Quinuclidine – Wikipedia,
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Related Products of 2386-57-4, 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. 2386-57-4, Name is Sodium methanesulfonate, SMILES is CS(=O)([O-])=O.[Na+], belongs to quinuclidines compound. In a article, author is HACKSELL, U, introduce new discover of the category.

QUINUCLIDIN-2-ENE – BASED MUSCARINIC ANTAGONISTS

A series of achiral 3-heteroaryl substituted quinuclidin-2-ene derivatives and related compounds have been synthesized by facile methods. The compounds were evaluated for muscarinic and antimuscarinic properties in receptor binding studies using (-)-[H-3]-QNB as the radioligand and ina functional assay using isolated guinea pig urinary bladder. 3-(2-Benzofuranyl)-quinuclidin-2-ene (15) displayed the highest M(1)-receptor affinity in the present series (K-i = 9.6 nM).

Related Products of 2386-57-4, 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 2386-57-4.

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Quinuclidine – Wikipedia,
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