Category: 123536-14-1

123536-14-1, In an article, published in an article,authors is Cappelli, Andrea, once mentioned the application 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.

Novel potent 5-HT3 receptor ligands based on the pyrrolidone structure: Synthesis, biological evaluation, and computational rationalization of the ligand-receptor interaction modalities

Novel conformationally constrained derivatives of classical 5-HT3 receptor antagonists were designed and synthesized with the aim of probing the central 5-HT3 receptor recognition site in a systematic way. The newly-synthesized compounds were tested for their potential ability to inhibit [3H]granisetron specific binding to 5-HT3 receptor in rat cortical membranes. These studies revealed subnanomolar affinity in some of the compounds under study. The most potent ligand in this series was found to be quinuclidine derivative (S)-7i, which showed an affinity comparable with that of the reference ligand granisetron. The potential 5-HT3 agonist/antagonist activity of some selected compounds was assessed in vitro on the 5-HT3 receptor-dependent [14C]guanidinium uptake in NG 108-15 cells. Both of the tropane derivatives tested in this functional assay (7a and 9a) showed antagonist properties, while the quinuclidine derivatives studied [the enantiomers of compounds 7i, 8g, and 9g, and compound (R)-8h] showed a full range of intrinsic efficacies. Therefore, the functional behavior of these 5-HT3 receptor ligands appears to be affected by the structural features of both the azabicyclo moiety and the heteroaromatic portion. In agreement with the data obtained on NG 108-15 cells, investigations on the 5-HT3 receptor-dependent Bezold-Jarisch reflex in urethane-anaesthetized rats confirmed the 5-HT3 receptor antagonist properties of compounds 7a and (S)-7i showing for these compounds ID50 values of 2.8 and 181 mug/kg, respectively. Finally, compounds 7a, (S)-7i and 9a (at the doses of 0.01, 1.0, and 0.01 mg/kg ip, respectively) prevented scopolamine-induced amnesia in the mouse passive avoidance test suggestive of a potential usefulness in cognitive disorders for these compounds. Qualitative and quantitative structure-affinity relationship studies were carried out by means of theoretical descriptors derived on a single structure and ad-hoc defined size and shape descriptors (indirect approach). The results showed to be useful in capturing information relevant to ligand-receptor interaction. Additional information derived by the analysis of the energy minimized 3-D structures of the ligand-receptor complexes (direct approach) suggested interesting mechanistic and methodological considerations on the binding mode multiplicity at the 5-HT3 receptors and on the degree of tolerance allowed in the alignment of molecules for the indirect approach, respectively.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H140N | ChemSpider

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 123536-14-1, name is (R)-3-Aminoquinuclidine dihydrochloride, introducing its new discovery. 123536-14-1

5-HT3 RECEPTOR MODULATORS, METHODS OF MAKING, AND USE THEREOF

Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.123536-14-1, you can also check out more blogs about123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H100N | ChemSpider

123536-14-1, 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 a patent, 123536-14-1, molecular formula is C7H16Cl2N2, introducing its new discovery.

PHARMACEUTICAL COMPOUNDS

The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H114N | ChemSpider

123536-14-1, 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 Manning, David D., mentioned the application of 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2

Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome

Serotonin type 3 (5-HT3) receptor partial agonists are being targeted as potential new drugs for the treatment of irritable bowel syndrome (IBS). Two new chemical series bearing indazole and indole cores have exhibited nanomolar binding affinity for the h5-HT3A receptor. A range of partial agonist activities in HEK cells heterologously expressing the h5-HT 3A receptor were measured for the indazole series. Excellent 5-HT3 receptor selectivity, favorable in vitro metabolic stability and CYP inhibition properties, and good oral in vivo potency in the murine von Bezold-Jarisch reflex model is exemplified thereby indicating the series to have potential utility as improved IBS agents.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H150N | ChemSpider

123536-14-1, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article, authors is Mould, Daniel P.£¬once mentioned of 123536-14-1

Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1

Inhibition of lysine specific demethylase 1 (LSD1) has been shown to induce the differentiation of leukemia stem cells in acute myeloid leukemia (AML). Irreversible inhibitors developed from the nonspecific inhibitor tranylcypromine have entered clinical trials; however, the development of effective reversible inhibitors has proved more challenging. Herein, we describe our efforts to identify reversible inhibitors of LSD1 from a high throughput screen and subsequent in silico modeling approaches. From a single hit (12) validated by biochemical and biophysical assays, we describe our efforts to develop acyclic scaffold-hops from GSK-690 (1). A further scaffold modification to a (4-cyanophenyl)glycinamide (e.g., 29a) led to the development of compound 32, with a Kd value of 32 nM and an EC50 value of 0.67 muM in a surrogate cellular biomarker assay. Moreover, this derivative does not display the same level of hERG liability as observed with 1 and represents a promising lead for further development.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H151N | ChemSpider

123536-14-1, Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 123536-14-1

NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Compounds of formula (I), wherein D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H105N | ChemSpider

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 Article, authors is Ouach, Aziz£¬once mentioned of 123536-14-1

Design of alpha7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies

We report here the synthesis of a large library of 1,2,3-triazole derivatives which were in vitro tested as alpha7 nAchR ligands. The SAR study revealed that several crucial factors are involved in the affinity of these compounds for alpha7 nAchR such as a (R) quinuclidine configuration and a mono C-3 quinuclidine substitution. The triazole ring was substituted by a phenyl ring bearing small OMe/CH2F groups or fluorine atom and by several heterocycles such as thiophenes, furanes, benzothiophenes or benzofuranes. Among the 30 derivatives tested, the two derivatives 10 and 39 with Ki in the nanomolar range were identified (2.3 and 3 nM respectively). They exhibited a strict selectivity toward the alpha4beta2 nicotinic receptor (up to 1 muM) but interacted with the 5HT3 receptors with Ki around 3 nM. Synthesis, SAR studies and a full description of the derivatives are reported.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.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 | C7H152N | ChemSpider

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 123536-14-1, molcular formula is C7H16Cl2N2, introducing its new discovery. , 123536-14-1

NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Compounds of formula (I), wherein D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 123536-14-1, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H106N | ChemSpider

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

Chiral polyoxometalate-based materials: From design syntheses to functional applications

Owing to the potential applications in catalysis, analytical chemistry, ion exchange, magnetism, biological chemistry and medicine, tremendous effort has been dedicated to exploring polyoxometalate (POM) chemistry. Chiral POM-based materials are particularly attractive due to the combination of the advantage of POMs with the importance of chirality. Nearly 100 chiral POM-based compounds were reported, which were mainly used as asymmetric catalysts, molecular recognition and nonlinear optical materials. In addition, the chirality within POM systems has attracted the attention of theoretical chemists and research was carried out to explore the origin of chirality by density functional theoretical methods. In this review, we summarize the developments of chiral POM-based materials, including their synthetic strategies, calculations on the origin of chirality and the relevant applications.

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 120-15-0!, 123536-14-1

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Quinuclidine – Wikipedia,
Quinuclidine | C7H144N | ChemSpider