Category: quinuclidine

Electric Literature 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.123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Patent£¬once mentioned of 123536-14-1

ALKALOID ESTER AND CARBAMATE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF

Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 123536-14-1, and how the biochemistry of the body works.Electric Literature of 123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H92N | ChemSpider

Application of 827-61-2, 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.In a document type is Article, and a compound is mentioned, 827-61-2, Quinuclidin-3-yl acetate, introducing its new discovery.

Structure-based discovery of prescription drugs that interact with the norepinephrine transporter, NET

The norepinephrine transporter (NET) transports norepinephrine from the synapse into presynaptic neurons, where norepinephrine regulates signaling pathways associated with cardiovascular effects and behavioral traits via binding to various receptors (e.g., beta2-adrenergic receptor). NET is a known target for a variety of prescription drugs, including antidepressants and psychostimulants, and may mediate off-target effects of other prescription drugs. Here, we identify prescription drugs that bind NET, using virtual ligand screening followed by experimental validation of predicted ligands. We began by constructing a comparative structural model of NET based on its alignment to the atomic structure of a prokaryotic NET homolog, the leucine transporter LeuT. The modeled binding site was validated by confirming that known NET ligands can be docked favorably compared to nonbinding molecules. We then computationally screened 6,436 drugs from the Kyoto Encyclopedia of Genes and Genomes (KEGG DRUG) against the NET model. Ten of the 18 high-scoring drugs tested experimentally were found to be NET inhibitors; five of these were chemically novel ligands of NET. These results may rationalize the efficacy of several sympathetic (tuaminoheptane) and antidepressant(tranylcypromine) drugs, as well as side effects of diabetes (phenformin) and Alzheimer’s (talsaclidine) drugs. The observations highlight the utility of virtual screening against a comparative model, even when the target shares less than 30% sequence identity with its template structure and no known ligands in the primary binding site.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 827-61-2. In my other articles, you can also check out more blogs about 827-61-2

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Quinuclidine – Wikipedia,
Quinuclidine | C7H80N | ChemSpider

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, HPLC of Formula: C9H15NO2, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. HPLC of Formula: C9H15NO2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Article, authors is Primozie, Ines£¬once mentioned of HPLC of Formula: C9H15NO2

Influence of the acyl moiety on the hydrolysis of quinuclidinium esters catalyzed by butyrylcholinesterase

Eight chiral esters of quinuclidin-3-ol and butyric, acetic, pivalic and benzoic acid were synthesized as well as their racemic and chiral, quaternary N-benzyl derivatives. All racemic and chiral quaternary compounds were studied as substrates and/or inhibitors of horse serum butyrylcholinesterase (BChE). The best substrate for the enzyme was (R)-N-benzyl butyrate. The rates of hydrolysis decreased in order (R)-butyrate (R)-acetate (7-fold slower) < (R)-pivalate (8-fold slower) < (R)-benzoate (9-fold slower reaction), while (S)-N-benzyl esters were much poorer substrates (320 (butyrate)-4360-fold slower (pivalate) than the appropriate (R)-enantiomer). For all (S)-N-benzyl esters excluding (S)-N-benzyl acetate inhibition constants were determined (Ka = 3.3.60 mumol dm-3). The hydrolysis of racemic mixtures of N-benzyl esters proceeded 1.4 (for acetate)-5.1 (for benzoate) times slower than that of pure (R)-enantiomers of the corresponding concentrations due to the inhibition with (S)-enantiomers. Change of the acyl moiety of the substrate effected both activity and stereoselectivity of the BChE. A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about HPLC of Formula: C9H15NO2 Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H78N | ChemSpider

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like category: quinuclidine, Name is Quinuclidin-3-yl acetate. In a document type is Article, introducing its new discovery., category: quinuclidine

Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonists

The insect muscarinic acetylcholine receptor (mAChR) is evaluated as a potential target for insecticide action. The mammalian M2/M4-selective antagonist radioligand [3H]AF-DX 384 (a pirenzepine analogue) binds to Drosophila mAChR at a single high-affinity site identical to that for the nonselective antagonist [3H]quinuclidinyl benzilate (QNB) and with a pharmacological profile distinct from that of all mammalian mAChR subtypes. Three nonselective antagonists (QNB, scopolamine, and atropine) show the highest affinity (Ki = 0.5-2.4 nM) at the Drosophila target, and AF-DX 384 and M3-selective 4-DAMP (dimethyl-4-(diphenylacetoxy)piperidinium iodide) rank next in potency (Ki = 5-18 nM). Eleven muscarinic antagonists generally exhibit higher affinity than eight agonists. On injection into houseflies, the antagonists 4-DAMP and (S)-(+)-dimethindene produce suppressed movement, the agonist (methyloxadiazolyl)quinuclidine causes knockdown and tremors, and all of them inhibit [3H]-QNB binding ex vivo, indicating possible mAChR-mediated intoxication. The insect mAChR warrants continuing study in lead generation to discover novel insecticides.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H62N | ChemSpider

Related Products of 827-61-2, 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. 827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Review£¬once mentioned of 827-61-2

Synthetic Methods Driven by the Photoactivity of Electron Donor-Acceptor Complexes

The association of an electron-rich substrate with an electron-accepting molecule can generate a new molecular aggregate in the ground state, called an electron donor-acceptor (EDA) complex. Even when the two precursors do not absorb visible light, the resulting EDA complex often does. In 1952, Mulliken proposed a quantum-mechanical theory to rationalize the formation of such colored EDA complexes. However, and besides a few pioneering studies in the 20th century, it is only in the past few years that the EDA complex photochemistry has been recognized as a powerful strategy for expanding the potential of visible-light-driven radical synthetic chemistry. Here, we explain why this photochemical synthetic approach was overlooked for so long. We critically discuss the historical context, scientific reasons, serendipitous observations, and landmark discoveries that were essential for progress in the field. We also outline future directions and identify the key advances that are needed to fully exploit the potential of the EDA complex photochemistry.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 827-61-2. In my other articles, you can also check out more blogs about 827-61-2

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Quinuclidine – Wikipedia,
Quinuclidine | C7H51N | ChemSpider

Application of 123536-14-1, 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.In a document type is Patent, and a compound is mentioned, 123536-14-1, (R)-3-Aminoquinuclidine dihydrochloride, introducing its new discovery.

Preparation of S-(-)- and R-(+)-N-(quinuclidinyl-3)-amide

Optical active forms of the carboxylic acid amines of 3-aminoquinuclidine of formula (I), and the preparation thereof. These can be hydrolysed to the optical active forms of 3-aminoquinuclidine.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 123536-14-1. In my other articles, you can also check out more blogs about 123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H112N | ChemSpider

Synthetic Route of 5291-32-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.Synthetic Route of 5291-32-7, Name is APR-246, molecular formula is C10H17NO3. In a Article, authors is Saha, Manujendra N.£¬once mentioned of Synthetic Route of 5291-32-7

PRIMA-1Met/APR-246 displays high antitumor activity in multiple myeloma by induction of p73 and noxa

Targeting p53 by the small-molecule PRIMA-1Met/APR-246 has shown promising preclinical activity in various cancer types.However, the mechanism of PRIMA-1Met-induced apoptosis is not completely understood and its effect on multiple myeloma cells is unknown. In this study, we evaluated antitumor effect of PRIMA-1Met alone or its combination with current antimyeloma agents in multiple myeloma cell lines, patient samples, and a mouse xenograft model. Results of our study showed that PRIMA-1Met decreased the viability of multiple myeloma cells irrespective of p53 status, with limited cytotoxicity toward normal hematopoietic cells. Treatment of multiple myeloma cells with PRIMA-1Met resulted in induction of apoptosis, inhibition of colony formation, and migration. PRIMA-1Met restored wild-type conformation of mutant p53 and induced activation of p73 upregulating Noxa and downregulating Mcl-1 without significant modulation of p53 level. siRNAmediated silencing of p53 showed a little effect on apoptotic response of PRIMA-1Met, whereas knockdown of p73 led to substantial attenuation of apoptotic activity in multiple myeloma cells, indicating that PRIMA-1Met- induced apoptosis is, at least in part, p73-dependent.Importantly, PRIMA-1Met delayed tumor growth and prolonged survival of mice bearing multiple myeloma tumor. Furthermore, combined treatment of PRIMA-1Met with dexamethasone or doxorubicin displayed synergistic effects in both multiple myeloma cell lines and primary multiple myeloma samples. Consistent with our in vitro observations, cotreatment with PRIMA-1Met and dexamethasone resulted in enhanced antitumor activity in vivo. Our study for the first time shows antimyeloma activity of PRIMA-1Met and provides the rationale for its clinical evaluation in patients with multiple myeloma, including the high-risk group with p53 mutation/deletion. Mol Cancer Ther; 12(11); 2331-41.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about Synthetic Route of 5291-32-7

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Quinuclidine – Wikipedia,
Quinuclidine | C7H174N | ChemSpider

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

Comparison of the muscarinic receptor binding activity of some tertiary amines and their quaternary ammonium analogues

A series of tertiary amines and their N-methyl quaternary salts were examined for their ability to inhibit specific [3H]3-quinuclidinyl benzilate binding to rat brain muscarinic receptors. The more flexible tertiary amines, like dimethylaminoethyl acetate, were less potent than their respective quaternary ammonium analogues, while rigid tertiary amines, like aceclidine, were more potent than their quaternary derivatives. The competition curves of most of the compounds were adequately described by a two-site binding equation. A good correlation between pharmacological activity and the high-affinity dissociation constant was observed. The influence of pH in the competitive inhibition of [3H]3-quinuclidinyl benzilate binding by arecoline and scopolamine was also examined. The potency of these amines declined relative to that of their N-methyl derivatives as the pH increased from 8.90 to 9.0, suggesting that it is primarily the protonated form of arecoline and scopolamine which interacts with the muscarinic receptor.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! Read on for other articles about Safety of 3,6-Dichloropyridazine!, COA of Formula: C9H15NO2

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Quinuclidine – Wikipedia,
Quinuclidine | C7H56N | ChemSpider

Application of 123536-14-1, 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. 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Patent£¬once mentioned of 123536-14-1

2-indolizine Carbamoyl amine compound and its preparation and use (by machine translation)

The invention discloses a novel 2-indolizine formylamine derivative. The general formula of the novel 2-indolizine formylamine derivative is as shown in a formula (I), wherein the definition of R is specified in the specification. In addition, the invention also discloses a preparation method and a medicine composition of the compound. The 2-indolizine formylamine derivative disclosed by the invention has an acetylcholine alpha 7 receptor exciting effect. The formula (I) is as shown in the specification.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 123536-14-1. In my other articles, you can also check out more blogs about 123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H134N | ChemSpider

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Quality Control of (R)-3-Aminoquinuclidine dihydrochloride. Introducing a new discovery about Quality Control of (R)-3-Aminoquinuclidine dihydrochloride, Name is (R)-3-Aminoquinuclidine dihydrochloride

Synthesis of quinazoline-2,4-dione and naphthalimide derivatives as new 5-HT3 receptor antagonists

New potent 5-HT3 receptor antagonists have been designed from the naphthalimide moiety and a quinuclidine heterocycle and the structure-activity relationships are discussed here on the basis of the nature of the substituent on the aromatic system. The biological activity of the compounds was evaluated in binding assays with [3H]BRL-43694 and by inhibition of the Bezold-Jarisch reflex. Compound 22 with a 4-amino substituent was equipotent to the reference compounds. In contrast to the benzamide derivatives, the activity resides essentially in the (R) enantiomer (K(i) = 0.15 ¡À 0.05 nM, ID50 = 1.6 mug/kg/iv) and it is demonstrated that the additional carbonyl group is involved in the inversion of the enantioselectivity of the receptor. Conformational studies of (R)-22 demonstrated the presence of a locked structure with 4 minimal energy conformers which were compared to those of (S)-zacopride. The superimposition of the putative active conformers emphasized the presence of a second polar group in the binding site. The fluorescent properties of the compounds were studied and indicate that (R)-22 and its derivatives may be promising tools for the direct visualization of 5-HT3 receptors.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H148N | ChemSpider