Day: March 30, 2021

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 142-45-0, Name is Acetylenedicarboxylic Acid, formurla is C4H2O4. In a document, author is Huang, Mei, introducing its new discovery. COA of Formula: C4H2O4.

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.

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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 Ugawa, T, once mentioned the application of 6753-98-6, Name is (1E,4E,8E)-2,6,6,9-Tetramethylcycloundeca-1,4,8-triene, molecular formula is C15H24, molecular weight is 204.3511, MDL number is MFCD00042689, category is quinuclidines. Now introduce a scientific discovery about this category, Computed Properties of C15H24.

Experimental model of escape phenomenon in hamsters and the effectiveness of YM-53601 in the model

1 The aim of this study was to establish an experimental model of the escape phenomenon, in which plasma cholesterol, initially reduced by a 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase inhibitor such as pravastatin, increases again on long-term administration. We also evaluated the efficacy of YM-53601 ((E)-2-[2-fluoro-2- (quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a squalene synthase inhibitor, in this model. 2 Pravastatin inhibited cholesterol biosynthesis in hamster primary hepatocytes (IC50, 14 nM). After pre-treatment with pravastatin, in contrast, almost no effect on cholesterol biosynthesis was seen. 3 In hamsters fed a high fat diet, 3 mg kg(-1) pravastatin for 9 days decreased plasma non-HDL cholesterol (total cholesterol-high density lipoprotein cholesterol) (P<0.01), but this effect was lost between 17 and 27 days of treatment, accompanied by an increase in HMG-CoA reductase activity. No such increase in plasma non-HDL cholesterol was seen with YM-53601 at 30 mg kg(-1) after 9 (P<0.001), 17 (P<0.01) or 27 (P<0.001) days of treatment. Replacement of pravastatin with YM-53601 caused a decrease in plasma non-HDL cholesterol by 53% (P<0.001) and in HMG-CoA reductase activity. 4 This animal model thus satisfactorily replicates the escape phenomenon observed in humans and may therefore be useful in evaluation of lipid-lowering agents, specifically comparison of HMG-CoA reductase inhibitors. Further, YM-53601 may be useful in the treatment of hypercholesterolemia without induction of the escape phenomenon. 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 6753-98-6, Computed Properties of C15H24.

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

Synthetic Route of 611-10-9, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 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 Brown, GR, introduce new discover of the category.

Novel optimised quinuclidine squalene synthase inhibitors

Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol 1c, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral ED(50) of 1c, for the inhibition of rat cholesterol biosynthesis was 1.3+/-0.45 mg/kg and for the R-enantiomer 1m, 0.8+/-0.2 mg/kg, with the corresponding R-carboxylic acid 6a, being 0.9+/-0.25 mg/kg. (C) 1997 Elsevier Science Ltd. All rights reserved.

Synthetic Route of 611-10-9, 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 611-10-9.

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

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 HACKSELL, U, once mentioned the new application about 25952-53-8, Recommanded Product: 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride.

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).

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. Recommanded Product: 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride.

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

In an article, author is Prishchenko, A. A., once mentioned the application of 632-22-4, Name is 1,1,3,3-Tetramethylurea, molecular formula is C5H12N2O, molecular weight is 116.1616, MDL number is MFCD00008319, category is quinuclidines. Now introduce a scientific discovery about this category, Category: quinuclidines.

Addition of tris(trimethylsilyl) phosphite to quinuclidin-3-one and its carbocyclic analogs

Convenient methods of synthesis of functionalized phosphonic acids and their trimethylsilyl esters containing quinuclidine, adamantine, and bornane (camphane) moieties, involving reactions of tris(trimethylsilyl) phosphite with quinuclidin-3-one and its carbocyclic analogs.

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

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 294-62-2, Name is Cyclododecane, SMILES is C1CCCCCCCCCCC1, in an article , author is Navratil, O, once mentioned of 294-62-2, Computed Properties of C12H24.

Competitive extraction of some bases by carbollyl-cobaltate anion from water into chloroform

The bis[undecahydro-7,8-dicarbaundecaborato(2-)]cobaltate(1-) (X-) has been used for complementary study of its ionic associates with some cations of organic bases and quaternary salts. For the optimization of present analytical methods, quinuclidin-3-yl hydroxy(diphenyl)acetate, 1-(1-phenylcyclohexyl)piperidine, dibenzo[b,f][1,4]oxazepine and cocaine, were studied by competitive extraction method. X- labelled with Co-60 was used as carrier anion, triphenylmethane and azo dyes as competitive anions, The aqueous phase was 0.1 and 0.01 M HCl, the organic phase was chloroform. A comparison was made with earlier results obtained by extraction spectrophotometry.

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

79-39-0, Name is Methacrylamide, molecular formula is C4H7NO, belongs to quinuclidines compound, is a common compound. In a patnet, author is Brown, GR, once mentioned the new application about 79-39-0, Application In Synthesis of Methacrylamide.

Novel optimised quinuclidine squalene synthase inhibitors

Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol 1c, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral ED(50) of 1c, for the inhibition of rat cholesterol biosynthesis was 1.3+/-0.45 mg/kg and for the R-enantiomer 1m, 0.8+/-0.2 mg/kg, with the corresponding R-carboxylic acid 6a, being 0.9+/-0.25 mg/kg. (C) 1997 Elsevier Science Ltd. All rights reserved.

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

Synthetic Route of 147126-62-3, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 147126-62-3, Name is (2R,5R)-(1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate, SMILES is O=C(O[C@H]1[C@@H](CC[C@H](C1)C)C(C)C)[C@@H]2O[C@H](CS2)O, belongs to quinuclidines compound. In a article, author is Primozic, I, introduce new discover of the category.

Structural basis for selectivity of butyrylcholinesterase towards enantiomeric quinuclidin-3-yl benzoates: a quantum chemical study

In order to explain different rates of hydrolysis of (R)- and (S)-quinuclidin-3-yl benzoates and benzoylcholine catalyzed with butyrylcholinesterase, semiempirical PM3 calculations were performed with an assumed active site model of human BChE (20 amino acids). Contributions of different protein residues to the stabilization of Michaelis complexes and tetrahedral intermediates were analyzed. It was shown that the hydrolysis rates of quinuclidinium enantiomers were to an appreciable extent affected by the existence or absence of the hydrogen bond between the quinuclidinium N+-H group and the protein residues. Calculations indicated that the better stabilization of quinuclidinium moiety in the Michaelis complex than in the tetrahedral intermediate was the main reason for a greater barrier and a slower reaction rate of the (R)-enantiomer of quinuclidinium esters compared to benzoylcholine. In the case of (S)-enantiomer, the calculation indicated that the barrier to the substrate reorientation from a favourable, but non-productive binding to a productive one significantly influenced the rate of hydrolysis.

Synthetic Route of 147126-62-3, 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 147126-62-3 is helpful to your research.

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

Synthetic Route of 535-75-1, 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. 535-75-1, Name is Pipecolinic Acid, SMILES is O=C(C1NCCCC1)O, belongs to quinuclidines compound. In a article, author is Shchekotikhin, AE, introduce new discover of the category.

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.

Synthetic Route of 535-75-1, 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 535-75-1 is helpful to your research.

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

Reference of 13419-61-9, 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. 13419-61-9, Name is Sodium decane-1-sulfonate, SMILES is CCCCCCCCCCS(=O)([O-])=O.[Na+], belongs to quinuclidines compound. In a article, author is Dolle, F, introduce new discover of the category.

Highly efficient synthesis of [C-11]Me-QNB, a selective radioligand for the quantification of the cardiac muscarinic receptors using PET

Me-QNB (N-methyl-quinuclidin-3-yl benzilate or N-methyl-quinuclidin-3-yl diphenylhydroxy acetate) is a hydrophilic, non-metabolized and highly specific muscarinic acetylcholinergic antagonist. Using this quaternary ammonium derivative of QNB, labelled with carbon-11, a positron-emitting isotope (half-life : 20.4 minutes), the potential for quantification of myocardial muscarinic receptors in vivo using the high-resolution, sensitive and quantitative imaging technique PET (positron emission tomography) was previously demonstrated in dogs and validated in humans. In this paper, the radiosynthesis of carbon-11-labelled Me-QNB is investigated and oriented towards the preparation of multi milliCuries of radiotracer. Typically, using no-carrier-added [C-11]methyl triflate as the alkylating agent and 0.64 mg (1.89 mu mol) of QNB as precursor for labelling at 100 degreesC for 1 minute lead to a 48.5% +/- 10% (15 runs) decay-corrected radiochemical yield (based on [C-11]methyl triflate). 183 mCi (+/- 39) of [C-11]Me-QNB ([C-11]-1) could be synthesized in only 27 to 28 minutes after EOB and occasionally, up to 340 mCi of [C-11]Me-QNB ([C-11]-1) were obtained, corresponding to a 85% decay-corrected yield. The associated decay-corrected specific radioactivities obtained were 2658 mCi/mu mol (+/- 971) at EOB.

Reference of 13419-61-9, 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 13419-61-9.

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