Category: quinuclidine

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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

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

Discovery of fused heterocyclic carboxamide derivatives as novel alpha7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation

The alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) has emerged as a promising therapeutic target for schizophrenia. In our previous work, a novel series of alpha7-nAChR agonists bearing scaffold of indolizine were discovered. To explore the effect of aromaticity on the activity and find more active agents, herein, fused heterocyclic carboxamide derivatives were designed and synthesized in this study. Based on the evaluation by two-electrode voltage clamp in Xenopus oocytes, 27 of the synthesized compounds showed obvious agonism of alpha7 nAChR. Particularly, compounds 10a and 10e showed significantly higher Emax than EVP-6124. The result illustrated the importance of aromaticity to the activity of agonism. Compound 10a, which showed EC50 of 1.88 muM and Emax of 72.4%, was further characterized comprehensively, including co-application with type II positive allosteric modulator PNU-120596, selectivity with other closely related ligand-gated ion channel, etc. The results showed that 10a showed moderate selectivity over other subtypes such as alpha4beta2 and alpha3beta4 nAChR. 10a evoked alpha7-like currents that were inhibited by MLA and enhanced in the presence of the alpha7 PAM PNU-120596. The analysis of binding mode and understanding of structure-activity relationship provided insights to develop more potent novel alpha7-nAChR agonists.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H158N | ChemSpider

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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

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

3d Transition Metals for C-H Activation

C-H activation has surfaced as an increasingly powerful tool for molecular sciences, with notable applications to material sciences, crop protection, drug discovery, and pharmaceutical industries, among others. Despite major advances, the vast majority of these C-H functionalizations required precious 4d or 5d transition metal catalysts. Given the cost-effective and sustainable nature of earth-abundant first row transition metals, the development of less toxic, inexpensive 3d metal catalysts for C-H activation has gained considerable recent momentum as a significantly more environmentally-benign and economically-attractive alternative. Herein, we provide a comprehensive overview on first row transition metal catalysts for C-H activation until summer 2018.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H57N | ChemSpider

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of Quinuclidin-4-ylmethanamine, such as the rate of change in the concentration of reactants or products with time.In a article, authors is , mentioned the application of 67496-78-0, Name is Quinuclidin-4-ylmethanamine, molecular formula is C8H16N2

2 SUBSTITUTED CEPHEM COMPOUNDS

The compounds of formula (I) of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H19N | ChemSpider

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Application In Synthesis of APR-246. Introducing a new discovery about 5291-32-7, Name is APR-246

COMBINATION CANCER THERAPIES

Drug combinations of a heteroarotinoid (e.g., SHetA2), and an Azabicyclooctan-3-one derivative (e.g., PRIMA-1 or PRIMAMET) and/or, a CDK4/6 inhibitor (e.g., Palbociclib, Abemaciclib, or Ribociclib), which are synergistically-effective as anti-cancer treatments, and kits and methods of use of such drug combinations.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H162N | ChemSpider

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

Synthesis of (R) and (S)-3-aminoquinuclidine from 3-quinuclidinone and (S) and (R)-1-phenethylamine

The synthesis of (R) and (S)-3-amino quinuclidine, an important building block for the synthesis of chiral 5-HT3 serotonin receptor antagonists, is described. The key reaction is the reduction by NaBH4 of the imine prepared from the 3-quinuclidinone and chiral (S) or (R)-1-phenethylamine.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H147N | ChemSpider

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ACECLIDINE ISOMERS AND SCALEMIC MIXTURES THEREOF FOR THE TREATMENT OF PRESBYOPIA

The invention provides compositions containing aceclidine isomers and scalemic mixtures thereof for the treatment of presbyopia. The compositions optionally contain an alpha-adrenergic agonist, a cycloplegic agent, a cryoprotectant, a non-ionic surfactant and/or a viscosity enhancer.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H38N | ChemSpider

Reference of 67496-78-0, 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. 67496-78-0, Name is Quinuclidin-4-ylmethanamine, molecular formula is C8H16N2. In a Patent£¬once mentioned of 67496-78-0

INDOLONES USEFUL AS SEROTONERGIC AGENTS

This invention relates to compounds of the formula: STR1 which are useful as 5-HT 4 agonists or antagonists and 5-HT 3 antagonists.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Synthetic Route 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 Patent£¬once mentioned of 827-61-2

Process for preparing salt of hyaluronic acid with a pharmaceutically active substance

Pharmaceutical preparations for topical administration containing a pharmacologically active substance together with hyaluronic acid or a molecular weight fraction thereof. The hyaluronic acid may be in the form of the free acid or may be a salt with an alkali or alkaline earth metal, magnesium, aluminum or ammonium, or in the form of a salt with one or more pharmacologically active substances.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H34N | ChemSpider