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METHODS FOR TREATING MUSCULAR DYSTROPHIES

Provided herein are methods for treating and preventing a disease related to diminution or dysfunction of a dystrophin-related complex in a subject in need thereof, comprising administering to the subject a compound that increases sarcospan. Also provided herein are pharmaceutical compositions comprising a compound that increases sarcospan, or a pharmaceutically acceptable salt or ester thereof, useful for the treatments described herein.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H32N | ChemSpider

Simple exploration of Quinuclidin-3-yl acetate

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Drug release from porous matrixes based on natural polymers

Background: This review provides a report on recent advances in the field of drug release from matrixes made of natural polymers. Herein, the properties of natural polymers such as proteins and polysaccharides are discussed in general. Selected detailed examples of drug release profiles from biopolymer matrixes have also been collected from scientific literature and practical work, and commented on. In this review, the most common natural polymers, i.e. collagen, elastin, chitosan, hyaluronic acid and sodium alginate have been discussed as biopolymers that can be potentially applied in drug delivery systems. Methodology: The most rapidly developing field of the biomaterials science is the one dealing with their application as matrixes in drug release systems. Such systems show numerous advantages when compared to conventional ones. They improve medical treatment efficiency due to the fact that drugs are placed directly into the infected part. Moreover, the drug release systems reduce toxic reactions because the drug does not pass through the body and, as a result, does not affect the healthy tissues. Such systems also improve the patient?s comfort during the treatment. Result: Biocompatibility, bioresorbability and non-toxicity are the significant properties characteristic for natural polymers. Natural polymers can be used to obtain biomaterials which can further find their applications in the production of bones or soft tissues implants as well as dressing materials placed on damaged skin. Nevertheless, the disadvantages of biomaterials made of natural polymers, e.g., high solubility and low thermal stability, limit the range of their potential applications. Therefore, it is necessary to modify material properties by carrying out the cross-linking process. Conclusion: Recently, a rapidly growing interest in the use of porous materials as controlled drug delivery matrixes has been observed since they present several positive features. The drug release from polymeric matrixes is based on the carrier degradation process which depends on dissolving and diffusion processes. The selection of a polymeric matrix depends on its compatibility with the drug as well as the manufacturing process which needs to be considered. The proper adjustment of the drug release rate is necessary to obtain the best results during medical treatment. Numerous classes of hydrophilic as well as hydrophobic drugs can be released from polymeric matrixes which is beneficial to medical treatment. The research of different drug release systems has already been carried out, and the results can be found in scientific literature.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H65N | ChemSpider

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TREATMENT OF SEXUAL DYSFUNCTION AND FOR IMPROVED SEXUAL QUALITY OF LIFE

Compositions and methods for treating sexual dysfunction and enhancing sexual satisfaction using topical application of alpha-1 adrenergic receptor agonists, muscarinic acetylcholine receptor agonists, nicotinic acetylcholine receptor agonists, and cholinesterase inhibitors are disclosed.

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Quinuclidine | C7H36N | ChemSpider

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827-61-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Article, authors is Schlessinger, Avner£¬once mentioned of 827-61-2

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.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H80N | ChemSpider

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Synthesis of the optical isomers of a new anticholinergic drug, penehyclidine hydrochloride (8018)

A practical diastereoselective synthetic method for 8018 enantiopure isomers is described. The intramolecular asymmetric epoxidation of mono-sulfonate 4 was applied for the execution of the synthesis of the key chiral building block for the first time. The isomers were obtained with 70-76% yields in 99-100% ee.

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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 Review, the author is Gandeepan, Parthasarathy and a compound is mentioned, 827-61-2, Quinuclidin-3-yl acetate, introducing its new discovery. 827-61-2

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

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Process for preparing quinuclidine enantiomers

A new composition of matter, (+) 3-acetoxy- quinuclidine and its salts, ophthalmic compositions comprising this compound or any of its physiologically acceptable salts in a suitable carrier such as a phosphate buffer, and a process of preparation of the active ingredients, which comprises esterifying quinuclidinol so as to obtain racemic 3-lower-alkoxy quinuclidine, subjecting same to enzymatic hydrolysis by a cholinesterase so as to selectively hydrolyze the (-) isomer, separating the unchanged (+) lower-alkoxy quinuclidine, hydrolyzing the latter and esterifying it to the desired compound. Amongst various homolophes the preferred compound is (+)3-acetoxy quinuclidine as this is pharmaceutically the most potent one.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H43N | ChemSpider

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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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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 827-61-2, molcular formula is C9H15NO2, introducing its new discovery. , 827-61-2

Ophthalmic formulation of a selective cyclooxygenase-2 inhibitory drug

There is provided a pharmaceutical composition suitable for topical administration to an eye which contains a selective COX-2 inhibitory drug or nanoparticles of a drug of low water solubility, in a concentration effective for treatment and/or prophylaxis of a disorder in the eye, and one or more ophthalmically acceptable excipients that reduce rate of removal from the eye such that the composition has an effective residence time of about 2 to about 24 hours. Also provided is a method of treating and/or preventing a disorder in an eye, the method comprising administering to the eye a composition of the invention.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H44N | ChemSpider

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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 | C7H50N | ChemSpider