Month: May 2021

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, Like 22767-49-3, Name is Sodium pentane-1-sulfonate. In a document, author is Huang, Mei, introducing its new discovery. Name: Sodium pentane-1-sulfonate.

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.

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 22767-49-3, you can contact me at any time and look forward to more communication. Name: Sodium pentane-1-sulfonate.

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Quinuclidine – Wikipedia,
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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 Odzak, Renata, once mentioned the application of 6846-50-0, Name is 2,2,4-Trimethylpentane-1,3-diyl bis(2-methylpropanoate), molecular formula is C16H30O4, molecular weight is 286.41, MDL number is MFCD00059267, category is quinuclidine. Now introduce a scientific discovery about this category, Category: quinuclidines.

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.

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 6846-50-0, you can contact me at any time and look forward to more communication. Category: quinuclidines.

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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. 110-44-1, Name is Sorbic acid, molecular formula is C6H8O2, belongs to quinuclidine compound, is a common compound. In a patnet, author is Gu, Jianhui, once mentioned the new application about 110-44-1, COA of Formula: C6H8O2.

Convenient new synthesis of umeclidinium bromide

Umeclidinium bromide, a drug used for chronic obstructive pulmonary disease, is synthesized through a new intermediate of phenyl(quinuclidin-4-yl)methanone. This novel method with simple operation flow and cheap reagents, makes it suitable for scale up. The overall four-step process provides umeclidinium bromide in 29% yield and the purity up to 99.83%. The X-ray crystal structure of the drug molecule was first reported.

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 110-44-1, you can contact me at any time and look forward to more communication. COA of Formula: C6H8O2.

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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.116-26-7, Name is 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde, SMILES is O=CC1=C(C)C=CCC1(C)C, belongs to quinuclidine compound. In a document, author is NILSSON, BM, introduce the new discover, Name: 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde.

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 116-26-7. Name: 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde.

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Quinuclidine – Wikipedia,
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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. 116-26-7, Name is 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde, SMILES is O=CC1=C(C)C=CCC1(C)C, belongs to quinuclidine compound. In a document, author is Radl, S, introduce the new discover, Application In Synthesis of 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde.

Synthesis and antinociceptive activity of some 3-chlorophenyl- and 6-chloropyridin-2-yl derivatives

Derivatives of 2-chloro-6-(4-hydroxy-1-methylpiperidin-4-yl)pyridine (2b) were prepared and tested as analgesics. 2-Chloro-6-lithiopyridine treated with quinuclidin-3-one, 1-methylpyrrolidin-3-one, 2-(dimethylaminomethyl) cyclohexanone, and ethyl 1-methylpiperidin-4-ylcarboxylate provided the corresponding alcohols 5, 6, 13a, and 6-chloro-2-pyridyl 1l-methylpiperidin-4-yl ketone (9). The ketone was reduced with sodium borohydride or treated with methylmagnesium chloride or phenyllithium to provide the corresponding alcohols 11, 12a and 12b, respectively. 1-[4-(6-Chloro-2-pyridyl)1-methyrpiperidin-4-yl]1-methylethanol (4b) was prepared from 2-chloro-6-(1-methyl-1,2,5,6-tetrahydropyridin-4-yl)pyridine (14b) by treatment with butyllithium and acetone followed by reduction of intermediate 15b with sodium cyanoborohydride.

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 116-26-7, you can contact me at any time and look forward to more communication. Application In Synthesis of 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde.

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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. 13623-94-4, Name is 1,1-Bis(methylthio)-2-nitroethylene. In a pantent, once mentioned the new application about 13623-94-4, Formula: C4H7NO2S2.

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.

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 13623-94-4, you can contact me at any time and look forward to more communication. Formula: C4H7NO2S2.

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Quinuclidine – Wikipedia,
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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. 116-26-7, Name is 2,6,6-Trimethylcyclohexa-1,3-dienecarbaldehyde. In a pantent, once mentioned the new application about 116-26-7, Computed Properties of C10H14O.

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. 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 116-26-7, you can contact me at any time and look forward to more communication. Computed Properties of C10H14O.

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In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 105-50-0, Name is Diethyl 1,3-acetonedicarboxylate, SMILES is O=C(OCC)CC(CC(OCC)=O)=O, in an article , author is Koikov, LN, once mentioned of 105-50-0, SDS of cas: 105-50-0.

Oximes of quinuclidin-3-ones as nitric oxide donors

Oximes of quinuclidin-3-ones give NO under mild biomimetic oxidative conditions and activate soluble guanylate cyclase.

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 105-50-0, you can contact me at any time and look forward to more communication. SDS of cas: 105-50-0.

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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.13139-15-6, Name is Boc-L-Leucine, SMILES is CC(C)C[C@H](NC(OC(C)(C)C)=O)C(O)=O, belongs to quinuclidine compound. In a document, author is Kobayashi, S, introduce the new discover, COA of Formula: C11H21NO4.

Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: a Ca2+ mobilization study in monkey cells

We investigated the effects of the new muscarinic receptor antagonist solifenacin succinate [YM905; (+)(IS,3′ R)-quinuclidin-3′ -yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] and the current antimuscarinic drugs for the treatment of overactive bladder (oxybutynin, tolterodine and darifenacin) on intracellular Ca2+ mobilization in response to M-3 muscarinic receptor activation in bladder smooth muscle and submandibular gland cells isolated from Cynomolgus monkeys. Solifenacin concentration-dependently inhibited carbachol-induced Ca2+ mobilization, with affinity constant values (pKi) of 8.5+/-0.053 in bladder smooth muscle cells and 8.2+/-0.051 in submandibular gland cells (n=5). The pKi value of solifenacin was almost equivalent to the values of oxybutynin, tolterodine and darifenacin in bladder smooth muscle cells (8.7, 8.5 and 8.4, respectively), while being lower than those in submandibular gland cells (9.0, 8.7 and 8.8, respectively). The bladder-selectivity index (Ki ratio: submandibular gland/bladder) for solifenacin (2.1) was statistically higher, moreover, than those for oxybutynin, tolterodine and darifenacin (0.51, 0.65 and 0.46, respectively). These findings consequently indicate solifenacin’s unique profile in terms of its selectivity for bladder smooth muscle cells over salivary gland cells in non-human primates, relative to oxybutynin, tolterodine and darifenacin. Solifenacin may, therefore, confer a promising therapeutic advantage for reducing adverse effects, such as dry mouth, exhibited by current antimuscarinic therapy for overactive bladder. (C) 2003 Elsevier Inc. All rights reserved.

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 13139-15-6, you can contact me at any time and look forward to more communication. COA of Formula: C11H21NO4.

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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 Karolyi, Benedek Imre, once mentioned the application of 6728-26-3, Name is trans-2-Hexenal, molecular formula is C6H10O, molecular weight is 98.143, MDL number is MFCD00007008, category is quinuclidine. Now introduce a scientific discovery about this category, Formula: C6H10O.

Acylated mono-, bis- and tris- Cinchona-Based Amines Containing Ferrocene or Organic Residues: Synthesis, Structure and in Vitro Antitumor Activity on Selected Human Cancer Cell Lines

A series of novel functionalized mono-, bis-and tris-(S)-{[(2S,4R,8R)-8-ethyl-quinuclidin-2-yl](6-methoxyquinolin-4-yl)}methanamines including ferrocene-containing derivatives was obtained by the reaction of the precursor amine with a variety of acylation agents. Their in vitro antitumor activity was investigated against human leukemia (HL-60), human neuroblastoma (SH-SY5Y), human hepatoma (HepG2) and human breast cancer (MCF-7) cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)-assay and the 50% inhibitory concentration (IC50) values were determined. Our data indicate that the precursor amine has no antitumor activity in vitro, but the bis-methanamines with ureido-, thioureido and amide-type linkers display attractive in vitro cytotoxicity and cytostatic effects on HL-60, HepG2, MCF-7 and SH-SY5Y cells. Besides H-1- and C-13-NMR methods the structures of the new model compounds were also studied by DFT calculations.

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 6728-26-3, you can contact me at any time and look forward to more communication. Formula: C6H10O.

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Quinuclidine – Wikipedia,
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