Day: January 11, 2021

An article , which mentions SDS of cas: 827-61-2, molecular formula is C9H15NO2. The compound – Quinuclidin-3-yl acetate played an important role in people’s production and life., SDS of cas: 827-61-2

Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists

A series of 5-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6- tetrahydropyrimidines (7a-h) was synthesized for biological evaluation as selective agonists for M1 receptors coupled to phosphoinositide (PI) metabolism in the central nervous system. Each ligand bound with high affinity to muscarinic receptors from rat brain as measured by inhibition of [3H]-(R)-quinuclidinyl benzilate ([3H]-(R)-QNB) binding. 5-(3-Methyl- 1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine trifluoroacetate (CDD- 0098-J; 7a) displayed high affinity (IC50 = 2.7 ¡À 0.69 muM) and efficacy at muscarinic receptors coupled to PI metabolism in the rat cortex and hippocampus. Increasing the length of the alkyl substituent increased affinity for muscarinic receptors yet decreased activity in PI turnover assays. The hippocampal PI response of 7a was blocked by lower concentrations of pirenzepine (8) or by higher concentrations of either AF-DX 116 (9) or p- fluorohexahydrosiladifenidol (10), suggesting that at low concentrations 7a selectively stimulates PI turnover through M1 receptors.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H54N | ChemSpider

Synthetic Route of 827-61-2, An article , which mentions Synthetic Route of 827-61-2, molecular formula is C9H15NO2. The compound – Quinuclidin-3-yl acetate played an important role in people’s production and life.

Binding studies with [3H]cis-methyldioxolane in different tissues. Under certain conditions [3H]cis-methyldioxolane labels preferentially but not exclusively agonist high affinity states of muscarinic M2 receptors.

Special conditions–tricine buffer containing Ca2+ and Mg2+, 22 degrees C (TCM)–allow to label a much higher proportion of muscarinic receptors by [3H]cis-methyldioxolane (CD) than hitherto described (Vickroy et al. 1984a). Taking the maximum number of binding sites, Bmax, of [3H]QNB as 100%, Bmax of [3H]CD amounts to 83% in the rat heart instead of the reported 17%, 33% in the cerebral cortex instead of 6%, 20% in hippocampus and 55% in pons/medulla. In the salivary glands specific binding was negligible. The affinities of a number of muscarinic agonists and antagonists to [3H]CD and [3H]QNB binding sites in different tissues of the rat are compared. Apparent affinities of agonists are much higher in the [3H]CD system, affinities of antagonists are slightly higher in the [3H]QNB system. In both assay systems receptors of heart and pons/medulla membranes seem to have similar drug specificity. They differ somewhat from those in the cortex. Receptors in the salivary glands, however, seem to be completely different from those in the other three tissues. In the heart [3H]CD binding can be abolished almost completely by GppNHp. In the cortex about half of the [3H]CD binding is susceptible to GppNHp. The reduction of binding in the cortex is due to a change in Bmax and not in the dissociation constant KD. Competition of unlabelled pirenzepine with [3H]CD: In heart and pons/medulla only low affinity sites for pirenzepine (M2-receptors) are labelled by [3H]CD.(ABSTRACT TRUNCATED AT 250 WORDS)

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Quinuclidine – Wikipedia,
Quinuclidine | C7H50N | ChemSpider

Synthetic Route of 827-61-2, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 827-61-2, molcular formula is C9H15NO2, introducing its new discovery.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PRESBYOPIA

The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably use aceclidine separate or together with a cycloplegic agent and/or with a nonionic surfactant and viscosity enhancer, and or with low concentrations of a selective a-2 adrenergic receptor agonist.

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 827-61-2 is helpful to your research. Synthetic Route of 827-61-2

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Quinuclidine – Wikipedia,
Quinuclidine | C7H39N | ChemSpider

In an article, published in an article,authors is Bender, Aaron M., once mentioned the application of Recommanded Product: 827-61-2, Name is Quinuclidin-3-yl acetate,molecular formula is C9H15NO2, is a conventional compound. this article was the specific content is as follows. Recommanded Product: 827-61-2

Classics in Chemical Neuroscience: Xanomeline

Xanomeline (1) is an orthosteric muscarinic acetylcholine receptor (mAChR) agonist, often referred to as M1/M4-preferring, that received widespread attention for its clinical efficacy in schizophrenia and Alzheimer?s disease (AD) patients. Despite the compound?s promising initial clinical results, dose-limiting side effects limited further clinical development. While xanomeline, and related orthosteric muscarinic agonists, have yet to receive approval from the FDA for the treatment of these CNS disorders, interest in the compound?s unique M1/M4-preferring mechanism of action is ongoing in the field of chemical neuroscience. Specifically, the promising cognitive and behavioral effects of xanomeline in both schizophrenia and AD have spurred a renewed interest in the development of safer muscarinic ligands with improved subtype selectivity for either M1 or M4. This Review will address xanomeline?s overall importance in the field of neuroscience, with a specific focus on its chemical structure and synthesis, pharmacology, drug metabolism and pharmacokinetics (DMPK), and adverse effects.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H46N | ChemSpider

Application of 123536-14-1, An article , which mentions Application of 123536-14-1, molecular formula is C7H16Cl2N2. The compound – (R)-3-Aminoquinuclidine dihydrochloride played an important role in people’s production and life.

Dual organocatalysis: Asymmetric allylic-allylic alkylation of alpha,alpha-dicyanoalkenes and Morita-Baylis-Hillman carbonates

The unprecedented asymmetric allylic-allylic alkylation of alpha,alpha-dicyanoalkenes and Morita-Baylis-Hillman (MBH) carbonates were developed by catalyzing by a suitable chiral tertiary amine. The resulting multifunctional alkylation products could also serve as versatile intermediates for other synthetic transformations. The analogous catalysts show no catalytic activity in the model reaction due to steric activity. The alkylation reaction could be conducted at higher temperature in 1,2-dichloroethane (DCE) with little effect on the enantioselectivity. Excellent results are obtained by employing two equivalents of the MBH adduct and when 10% mol of (R)-BINOL is used. Mixtures of mono and double-allylic alkylation products are formed when symmetric alpha,alpha-dicyanoalkenes are applied. It is also found that the double-allylic alkylation adducts with four stereogenic centers could be isolated as single diasteromers with remarkable ee values.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H141N | ChemSpider

Related Products of 123536-14-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.Related Products of 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article, authors is Sarasamkan, Jiradanai£¬once mentioned of Related Products of 123536-14-1

Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds

The novel quinuclidine anti-1,2,3-triazole derivatives T1-T6 were designed based on the structure of QND8. The binding studies revealed that the stereochemistry at the C3 position of the quinuclidine scaffold plays an important role in the nAChR subtype selectivity. Whereas the (R)-enantiomers are selective to alpha7 over alpha4beta2 (by factors of 44-225) and to a smaller degree over alpha3beta4 (3-33), their (S)-counterparts prefer alpha3beta4 over alpha4beta2 (62-237) as well as over alpha7 (5-294). The (R)-derivatives were highly selective to alpha7 over alpha3beta4 subtypes compared to (RS)- and (R)-QND8. The (S)-enantiomers are 5-10 times more selective to alpha4beta2 than their (R) forms. The overall strongest affinity is observed for the (S)-enantiomer binding to alpha3beta4 (Ki, 2.25-19.5 nM) followed by their (R)-counterpart binding to alpha7 (Ki, 22.5-117 nM), with a significantly weaker (S)-enantiomer binding to alpha4beta2 (Ki, 414-1980 nM) still above the very weak respective (R)-analogue affinity (Ki, 5059-10436 nM).

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Quinuclidine – Wikipedia,
Quinuclidine | C7H154N | ChemSpider

Reference of 827-61-2, 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.In a article, authors is Mali, Suraj N., mentioned the application of Reference of 827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2

In Silico Appraisal, Synthesis, Antibacterial Screening and DNA Cleavage for 1,2,5-thiadiazole Derivative

Background: Thiadiazole not only acts as ?hydrogen binding domain? and ?two-electron donor system? but also as constrained pharmacophore. Methods: The maleate salt of 2-((2-hydroxy-3-((4-morpholino-1, 2,5-thiadiazol-3-yl) oxy) propyl) amino)- 2-methylpropan-1-ol (TML-Hydroxy)(4) has been synthesized. This methodology involves preparation of 4-morpholino-1, 2,5-thiadiazol-3-ol by hydroxylation of 4-(4-chloro-1, 2,5-thiadiazol-3-yl) morpholine followed by condensation with 2-(chloromethyl) oxirane to afford 4-(4-(oxiran-2-ylmethoxy)-1,2,5-thiadiazol- 3-yl) morpholine. Oxirane ring of this compound was opened by treating with 2-amino-2-methyl propan-1- ol to afford the target compound TML-Hydroxy. Structures of the synthesized compounds have been elucidated by NMR, MASS, FTIR spectroscopy. Results: The DSC study clearly showed that the compound 4-maleate salt is crystalline in nature. In vitro antibacterial inhibition and little potential for DNA cleavage of the compound 4 were explored. We extended our study to explore the inhibition mechanism by conducting molecular docking, ADMET and molecular dynamics analysis by using Schroedinger. The molecular docking for compound 4 showed better interactions with target 3IVX with docking score of -8.508 kcal/mol with respect to standard ciprofloxacin (docking score= -3.879 kcal/mol). TML-Hydroxy was obtained in silico as non-carcinogenic and non-AMES toxic with good percent human oral absorption profile (69.639%). TML-Hydroxy showed the moderate inhibition against Mycobacteria tuberculosis with MIC 25.00 mug/mL as well as moderate inhibition against S. aureus, Bacillus sps, K. Pneumoniae and E. coli species. Conclusion: In view of the importance of the 1,2,5-thiadiazole moiety involved, this study would pave the way for future development of more effective analogs for applications in medicinal field.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H70N | ChemSpider

Related Products of 67496-78-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, Related Products of 67496-78-0, molcular formula is C8H16N2, introducing its new discovery.

Pyrimido[5,4]-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof

Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[1-methyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine, and 4-[(3-Chloro-4-fluorophenyl)amino]-6-[trans-4-dimethyl-aminocycohexylamino]pyrimido[5,4-d]pyrimidine.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H16N | ChemSpider

Electric Literature of 827-61-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.Electric Literature of 827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a article£¬once mentioned of Electric Literature of 827-61-2

New Strategies for the Transition-Metal Catalyzed Synthesis of Aliphatic Amines

Transition-metal catalyzed reactions that are able to construct complex aliphatic amines from simple, readily available feedstocks have become a cornerstone of modern synthetic organic chemistry. In light of the ever-increasing importance of aliphatic amines across the range of chemical sciences, this review aims to provide a concise overview of modern transition-metal catalyzed approaches to alkylamine synthesis and their functionalization. Selected examples of amine bond forming reactions include: (a) hydroamination and hydroaminoalkylation, (b) transition-metal catalyzed C(sp3)-H functionalization, and (c) transition-metal catalyzed visible-light-mediated light photoredox catalysis.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H86N | ChemSpider

Related Products of 123536-14-1, In an article, published in an article,authors is Bourdin, Celine M., once mentioned the application of Related Products of 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride,molecular formula is C7H16Cl2N2, is a conventional compound. this article was the specific content is as follows.

Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammalian alpha7 nicotinic acetylcholine receptor

Abstract From quaternarization of quinuclidine enantiomers of 2-fluoro benzamide LMA10203 in dichloromethane, the corresponding N-chloromethyl derivatives LMA10227 and LMA10228 were obtained. Here, we compared the agonist action of known zacopride and its 2-fluoro benzamide analogues, LMA10203, LMA10227 and LMA10228 against mammalian homomeric alpha7 nicotinic acetylcholine receptor expressed in Xenopus oocytes. We found that LMA10203 was a partial agonist of alpha7 receptor with a pEC50 value of 4.25 ¡À 0.06 muM whereas LMA10227 and LMA10228 were poorly active on alpha7 homomeric nicotinic receptor. LMA10227 and LMA10228 were identified as antagonists of acetylcholine-induced currents with IC50 values of 28.4 muM and 39.3 muM whereas LMA10203 and zacopride possessed IC50 values of 8.07 muM and 7.04 muM, respectively. Moreover, despite their IC50 values, LMA10227 was the most potent inhibitor of nicotine-induced current amplitudes (65.7 ¡À 2.1% inhibition). LMA10203 and LMA10228 had the same inhibitory effects (26.5 ¡À 7.5% and 33.2 ¡À 4.1%, respectively), whereas zacopride had no significant inhibitory effect (4.37 ¡À 4%) on nicotine-induced responses. Our results revealed different pharmacological properties between the four compounds on acetylcholine and nicotine currents. The mode of action of benzamide compounds may need to be reinterpreted with respect to the potential role of alpha7 receptor.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H137N | ChemSpider