Tag: M.W=200-300

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Formula: C12H19NO4S, 253168-94-4, Name is 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine, SMILES is O=S(CC(N)C1=CC=C(OC)C(OCC)=C1)(C)=O, in an article , author is Dolle, F, once mentioned of 253168-94-4.

Highly efficient synthesis of [C-11]Me-QNB, a selective radioligand for the quantification of the cardiac muscarinic receptors using PET

Me-QNB (N-methyl-quinuclidin-3-yl benzilate or N-methyl-quinuclidin-3-yl diphenylhydroxy acetate) is a hydrophilic, non-metabolized and highly specific muscarinic acetylcholinergic antagonist. Using this quaternary ammonium derivative of QNB, labelled with carbon-11, a positron-emitting isotope (half-life : 20.4 minutes), the potential for quantification of myocardial muscarinic receptors in vivo using the high-resolution, sensitive and quantitative imaging technique PET (positron emission tomography) was previously demonstrated in dogs and validated in humans. In this paper, the radiosynthesis of carbon-11-labelled Me-QNB is investigated and oriented towards the preparation of multi milliCuries of radiotracer. Typically, using no-carrier-added [C-11]methyl triflate as the alkylating agent and 0.64 mg (1.89 mu mol) of QNB as precursor for labelling at 100 degreesC for 1 minute lead to a 48.5% +/- 10% (15 runs) decay-corrected radiochemical yield (based on [C-11]methyl triflate). 183 mCi (+/- 39) of [C-11]Me-QNB ([C-11]-1) could be synthesized in only 27 to 28 minutes after EOB and occasionally, up to 340 mCi of [C-11]Me-QNB ([C-11]-1) were obtained, corresponding to a 85% decay-corrected yield. The associated decay-corrected specific radioactivities obtained were 2658 mCi/mu mol (+/- 971) at EOB.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 253168-94-4, you can contact me at any time and look forward to more communication. Formula: C12H19NO4S.

Reference:
Quinuclidine – Wikipedia,
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In an article, author is Herschorn, Sender, once mentioned the application of 301-02-0, Name is Oleamide, molecular formula is C18H35NO, molecular weight is 281.4766, MDL number is MFCD00053638, category is quinuclidines. Now introduce a scientific discovery about this category, Computed Properties of C18H35NO.

Tolerability of 5 mg Solifenacin Once Daily Versus 5 mg Oxybutynin Immediate Release 3 Times Daily: Results of the VECTOR Trial

Purpose: Although antimuscarinic treatment is indicated for overactive bladder, many patients discontinue it because of dry mouth. Of available antimuscarinics oxybutynin is associated with the highest dry mouth rate. We compared the safety and tolerability of 5 mg solifenacin vs 15 mg oxybutynin immediate release. Materials and Methods: At 12 Canadian centers a total of 132 patients with overactive bladder symptoms (greater than 1 urgency episode per 24 hours, and 8 or greater micturitions per 24 hours) were randomized to 5 mg solifenacin once daily or 5 mg oxybutynin 3 times daily for 8 weeks. The primary end point was the incidence and severity of dry mouth reported after direct questioning. Efficacy end points (3-day diary documented changes in urgency, frequency, incontinence, nocturia and voided volume), and changes on the Patient Perception of Bladder Condition scale and the Overactive Bladder Questionnaire were evaluated secondarily. Results: Of patients on solifenacin vs oxybutynin immediate release 35% vs 83% reported dry mouth (p <0.0001). Of patients reporting dry mouth severity was graded moderate by 13% and 42% of those on solifenacin and oxybutynin immediate release, and severe by 13% and 28%, respectively (p = 0.001). Patients in each group showed improvements in efficacy end points, and Patient Perception of Bladder Condition scale and Overactive Bladder Questionnaire scores from baseline to treatment end. Conclusions: Significantly fewer patients on 5 mg solifenacin once daily reported dry mouth vs those receiving 5 mg oxybutynin immediate release 3 times daily. Significantly fewer patients on solifenacin reported moderate/severe dry mouth. Significantly fewer patients on solifenacin withdrew from study due to dry mouth and there were significantly fewer overall adverse events. Solifenacin and oxybutynin immediate release were efficacious in decreasing efficacy end points, and improved Patient Perception of Bladder Condition scale and Overactive Bladder Questionnaire results from baseline to treatment end. Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 301-02-0, Computed Properties of C18H35NO.

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25265-77-4, Name is 2,2,4-Trimethyl-1,3-pentanediol 1-monoisobutyrate, molecular formula is C12H24O3, belongs to quinuclidines compound, is a common compound. In a patnet, author is Klimova, EI, once mentioned the new application about 25265-77-4, HPLC of Formula: C12H24O3.

Stereospecific formation of polycyclic ferrocenyldihydropyrazoles based on Z- and E-isomeric ferrocenyl- substituted alpha,beta-unsaturated ketones of the heterocyclic series

The reactions of E- and Z-isomeric 2-(ferrocenylmethylidene)quinuclidin-3-one, 1-methyl-3-(ferrocenylmethylidene)piperidin-4-one, and 2-(ferrocenylmethylidene)tropinone with hydrazine proceed stereospecifically to form the same diastereomeric polycyclic ferrocenyldihydropyrazoles regardless of the geometrical configuration of the starting alpha,beta -unsaturated ketones. The structure of the trans-diastereomer of 4-acetyl-3-ferrocenyl-1,4,5-triazatricyclo[5.2.2.0(2,6)]undec-5-ene was established by X-ray diffraction analysis.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 25265-77-4. The above is the message from the blog manager. HPLC of Formula: C12H24O3.

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Reference of 957-68-6, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 957-68-6, Name is 7-Aminocephalosporanic acid, SMILES is CC(OCC(CS[C@@]([H])(N12)[C@H](N)C2=O)=C1C(O)=O)=O, belongs to quinuclidines compound. In a article, author is Lopez-Rodriguez, ML, introduce new discover of the category.

Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT3 receptors

A new series of azabicyclic benzimidazole-4-carboxamides 2-21 and -carboxylates 22-30 were synthesized and evaluated for binding affinity at serotoninergic 5-HT3 and 5-HT4 receptors in the CNS. Most of the synthesized compounds exhibited high or very high affinity for the 5-HT3 binding site and low to no significant affinity for the 5-HT4 receptor. SAR observations indicated that a halogen atom at the Ii-position and a nitro group at the 7-position of the benzimidazole ring is the best substitution pattern for 5-HT3 affinity and 5-HT3/5-HT4 selectivity, as well as no substitution in this ring. (S)-(-)-N-(Quinuclidin-3-yl)benzimidazo-4-carboxamides 2, 8, and 14 bound at central 5-HT3 sites with high affinity (K-i = 2.6, 0.13, and 1.7 nM, respectively) and excellent selectivity over serotonin 5-HT4 and 5-HT1A receptors (K-i > 1000-10000 dM). Furthermore, these new 5-HT3 receptor ligands were pharmacologically characterized as potent and selective 5-HT3 antagonists in the isolated guinea pig ileum (pA(2) = 9.6, 9.9, and 9.1, respectively).

Reference of 957-68-6, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 957-68-6.

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Quinuclidine – Wikipedia,
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Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 13139-15-6, Name is Boc-L-Leucine, molecular formula is , belongs to quinuclidines compound. In a document, author is Kobayashi, S, HPLC of Formula: C11H21NO4.

Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: a Ca2+ mobilization study in monkey cells

We investigated the effects of the new muscarinic receptor antagonist solifenacin succinate [YM905; (+)(IS,3′ R)-quinuclidin-3′ -yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] and the current antimuscarinic drugs for the treatment of overactive bladder (oxybutynin, tolterodine and darifenacin) on intracellular Ca2+ mobilization in response to M-3 muscarinic receptor activation in bladder smooth muscle and submandibular gland cells isolated from Cynomolgus monkeys. Solifenacin concentration-dependently inhibited carbachol-induced Ca2+ mobilization, with affinity constant values (pKi) of 8.5+/-0.053 in bladder smooth muscle cells and 8.2+/-0.051 in submandibular gland cells (n=5). The pKi value of solifenacin was almost equivalent to the values of oxybutynin, tolterodine and darifenacin in bladder smooth muscle cells (8.7, 8.5 and 8.4, respectively), while being lower than those in submandibular gland cells (9.0, 8.7 and 8.8, respectively). The bladder-selectivity index (Ki ratio: submandibular gland/bladder) for solifenacin (2.1) was statistically higher, moreover, than those for oxybutynin, tolterodine and darifenacin (0.51, 0.65 and 0.46, respectively). These findings consequently indicate solifenacin’s unique profile in terms of its selectivity for bladder smooth muscle cells over salivary gland cells in non-human primates, relative to oxybutynin, tolterodine and darifenacin. Solifenacin may, therefore, confer a promising therapeutic advantage for reducing adverse effects, such as dry mouth, exhibited by current antimuscarinic therapy for overactive bladder. (C) 2003 Elsevier Inc. All rights reserved.

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Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Electric Literature of 2425-77-6, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 2425-77-6, Name is 2-Hexyl-1-decanol, SMILES is CCCCCCCCC(CCCCCC)CO, belongs to quinuclidines compound. In a article, author is Boskovic, Perica, introduce new discover of the category.

The Aggregation Behavior and Antioxidative Activity of Amphiphilic Surfactants Based on Quinuclidin-3-ol

The self-aggregation and thermodynamic properties of three cationic quaternary ammonium surfactants were investigated. The physicochemical properties of compounds containing quinuclidin-3-ol with even number of carbon atoms (10, 12, and 14) in the hydrophobic tail were measured by conductivity, dynamic light scattering (DLS), and Zeta-potential measurements. DLS and Zeta-potential measurements show a similar size distribution for all surfactants with excellent uniformity, and Zeta-potential increases significantly with increase in the size of hydrocarbon tail. The critical micelle concentration (CMC) and the degree of micelle ionization (beta) were determined using conductivity measurements. The CMC values of surfactants were found to be between 3.4 and 23.8 x 10(-3) M. The standard Gibbs free energy (Delta Gmico) was derived from conductivity measurements and suggests that surfactants containing longer chains spontaneously form micelles. The antioxidative properties of these cationic surfactants were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) assays. Among the tested samples, N-tetradecyl-3-hydroxyquinuclidinium bromide (QOH-C14) exhibited the highest antioxidative potential (388.30 nmol (TE) equivalents mL(-1)), which was further investigated by the DNA nicking assay.

Electric Literature of 2425-77-6, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 2425-77-6.

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Quinuclidine – Wikipedia,
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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 5324-84-5, Name is Sodium octane-1-sulfonate, SMILES is CCCCCCCCS(=O)([O-])=O.[Na+], in an article , author is Tudosie, Mihail S., once mentioned of 5324-84-5, Application In Synthesis of Sodium octane-1-sulfonate.

New synthesized oximes active in nerve agents’ hazards

Object: The aim of the study is to select the most active new imidazolium-quinuclidinumoxime, from some similar chemical compounds synthesized in our chemistry department, with sufficient efficacy to decrease the acute toxicity of neurotoxic organophosphates known as nerve agents. Method: The experimental study consist in vivo testing the antidotal efficacy of obidoxime and of selected imidazolium oximes synthesized in our chemistry department. Each oxime was included, by equimolar replacing the obidoxime, in an antidotal formula, which also contains atropine. The above mentioned formula containing atropine and obidoxime was used as reference. The protective ratio, defined as the ratio between the lethal median dose of the poisoned and treated study group and the median lethal dose (LD50) of the poisoned and untreated study groups was one of the used parameters in order to select a new active chemical structure in counteracting the neurotoxic organophosphorus compounds acute toxicity. Another studied parameter was the erythrocyte acetylcholinesterase value measured in whole blood 24 hours after exposure. Results: The protective ratio against an organophosphorus compound were the follow: obidoxime chloride: 2; 1,3dimethyl-2-hydroxyethyl-imidazolyliodide: 1,75;3-oxime-[3-(2-hidroxyimino-methyl-1-imidazolyl-)-2oxapropyl] quinuclidin-dichl-oride: 2,5; 1-methyl-quinuclidin-3-iodide: 1,5. The erythrocyte acetycholinesterase main values were the following: the unpoisoned and untreated study group: 3,45 +/- 0,13mmol/dl; the poisoned and untreated study group: 0,89 +/- 0,09 mmol/dl; the poisoned and 3oxime-[3-(2-hidroxyimino-methyl-1-imidazolyl-)-2oxapropyl]quinuclidindichloride treated study group: 2,89 +/- 0,11 mmol/dl; the poisoned and obidoxime treated study group: 2,53 +/- 0,15 mmol/dl. Conclusions: 3-oxime-[3-(2-hidroxyimino-methyl-1-imidazolyl-)-2oxapropyl] quinuclidindichloride synthesized in our chemistry department, has shown a better protective ratio and a more prolonged surviving time than the reference (obidoxime). It has shown the best AChE reactivation of all the synthetized compounds. This compound can be a cheap and good option for replacing obidoxime in the antidotal formula active in nerve agent exposure.

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Quinuclidine – Wikipedia,
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In an article, author is Kobayashi, S, once mentioned the application of 112-80-1, Name is Oleic acid, molecular formula is C18H34O2, molecular weight is 282.4614, MDL number is MFCD00064242, category is quinuclidines. Now introduce a scientific discovery about this category, Product Details of 112-80-1.

Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: a Ca2+ mobilization study in monkey cells

We investigated the effects of the new muscarinic receptor antagonist solifenacin succinate [YM905; (+)(IS,3′ R)-quinuclidin-3′ -yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] and the current antimuscarinic drugs for the treatment of overactive bladder (oxybutynin, tolterodine and darifenacin) on intracellular Ca2+ mobilization in response to M-3 muscarinic receptor activation in bladder smooth muscle and submandibular gland cells isolated from Cynomolgus monkeys. Solifenacin concentration-dependently inhibited carbachol-induced Ca2+ mobilization, with affinity constant values (pKi) of 8.5+/-0.053 in bladder smooth muscle cells and 8.2+/-0.051 in submandibular gland cells (n=5). The pKi value of solifenacin was almost equivalent to the values of oxybutynin, tolterodine and darifenacin in bladder smooth muscle cells (8.7, 8.5 and 8.4, respectively), while being lower than those in submandibular gland cells (9.0, 8.7 and 8.8, respectively). The bladder-selectivity index (Ki ratio: submandibular gland/bladder) for solifenacin (2.1) was statistically higher, moreover, than those for oxybutynin, tolterodine and darifenacin (0.51, 0.65 and 0.46, respectively). These findings consequently indicate solifenacin’s unique profile in terms of its selectivity for bladder smooth muscle cells over salivary gland cells in non-human primates, relative to oxybutynin, tolterodine and darifenacin. Solifenacin may, therefore, confer a promising therapeutic advantage for reducing adverse effects, such as dry mouth, exhibited by current antimuscarinic therapy for overactive bladder. (C) 2003 Elsevier Inc. All rights reserved.

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Quinuclidine – Wikipedia,
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Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 112-62-9, Name is Methyl oleate, SMILES is CCCCCCCC/C=CCCCCCCCC(OC)=O, belongs to quinuclidines compound. In a document, author is Ohtake, A, introduce the new discover, HPLC of Formula: C19H36O2.

In vitro and in vivo tissue selectivity profile of solifenacin succinate (YM905) for urinary bladder over salivary gland in rats

Solifenacin succinate [YM905; (+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate] is a new muscarinic receptor antagonist developed for the treatment of overactive bladder. The aim of the present study was to evaluate the in vitro and in vivo bladder selectivity profile of solifenacin over salivary gland in the same animal species, and to compare the results with those obtained for tolterodine, oxybutynin, darifenacin and atropine. Solifenacin and the other antimuscarinic drugs inhibited carbachol-induced increases in intracellular Ca2+ levels in bladder smooth muscle cells and salivary gland cells isolated from rats in a concentration-dependent manner. The inhibitory effect of solifenacin for bladder smooth muscle cells (pK(i) = 8.12) was 3.6-fold more potent than that for salivary gland cells (pK(i) = 7.57). In contrast, the inhibitory effects of the other antimuscarinic drugs for bladder smooth muscle cells were 1.7- to 2.2-fold more potent than those for salivary gland cells. In anesthetized rats, solifenacin dose-dependently inhibited carbachol-induced intravesical pressure elevation and salivary secretion, and exhibited functional selectivity (3.7- to 6.5-fold) for urinary bladder over salivary gland. Tolterodine was also 2.2- to 2.4-fold more selective in inhibition of bladder response. In contrast, oxybutynin, darifenacin and atropine did not show functional selectivity for urinary bladder. These results indicate that solifenacin exerts greater selectivity for urinary bladder over salivary gland than tolterodine, oxybutynin, darifenacin and atropine, and may consequently provide symptomatic benefit in the treatment of overactive bladder with less dry mouth than currently used antimuscarinic drugs. (C) 2004 Elsevier B.V. All rights reserved.

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 112-62-9 is helpful to your research. HPLC of Formula: C19H36O2.

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Quinuclidine – Wikipedia,
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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. 2425-77-6, Name is 2-Hexyl-1-decanol, molecular formula is C16H34O. In an article, author is Primozic, Ines,once mentioned of 2425-77-6, Product Details of 2425-77-6.

Preparation of Novel meta- and para-Substituted N-Benzyl Protected Quinuclidine Esters and Their Resolution with Butyrylcholinesterase

Since the optically active quinuclidin-3-ol is an important intermediate in the preparation of physiologically or pharmacologically active compounds, a new biocatalytic method for the production of chiral quinuclidin-3-ols was examined. Butyrylcholinesterase (BChE; EC 3.1.1.8) was chosen as a biocatalyst in a preparative kinetic resolution of enantiomers. A series of racemic, (R)- and (S)-esters of quinuclidin-3-ol and acetic, benzoic, phthalic and isonicotinic acids were synthesized, as well as their racemic quaternary N-benzyl, meta- and para-N-bromo and N-methylbenzyl derivatives. After the resolution, all N-benzyl protected groups were successfully removed by catalytic transfer hydrogenation with ammonium formate (10% Pd-C). Hydrolyses studies with BChE confirmed that (R)-enantiomers of the prepared esters are much better substrates for the enzyme than (S)-enantiomers. Introduction of bromine atom or methyl group in the meta or para position of the benzyl moiety resulted in a considerable improvement of the stereoselectivity compared to the non-substituted compounds. Optically pure quinuclidin-3-ols were prepared in high yields and enantiopurity by the usage of various N-benzyl protected groups and BChE as a biocatalyst.

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Quinuclidine – Wikipedia,
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