Tag: M.W=200-300

The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. In a document, author is Johansson, G, introducing its new discovery. Product Details of 112-80-1.

A series of 25 derivatives of the muscarinic antagonist 3-(2-furanyl)quinuclidin-2-ene (4) was synthesized and evaluated for muscarinic and antimuscarinic properties. Substitution at all three positions of the furan ring has been investigated. The affinities of the new compounds were determined by competition experiments in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate as the radioligand, and the antimuscarinic potency was determined in a functional assay on isolated guinea pig urinary bladder using carbachol as the agonist. Several of the novel derivatives displayed high muscarinic affinities. Whereas the affinity of lead compound 4 for cortical muscarinic receptors is moderate (K-i 300 nM), it is much higher for the 6-methyl (49; K-i = 12 nM), 5-ethyl (52; K-i = 7.4 nM), 5-bromo (33; K-i = 6.4 nM), and 3-phenyl (49; K-i = 2.8 nM) substituted derivatives. The substituent-induced increases in affinity do not appear to be additive as a 5-bromo-3-phenyl (54), and a 5-methyl-3-phenyl (55) substitution pattern only slightly increases affinity (K-i = 1.55 and 2.39 nM, respectively). The conformational preferences of the 3-phenyl (49) and 5-phenyl (51) derivatives were studied by X-ray crystallography and molecular mechanics calculations. Because of the observed high affinity of 49, a series of 16 meta-and para-substituted analogues of 49 was synthesized and tested. derivative (68) exhibited more than 10-fold improvement in affinity as compared to 49. The structure-activity relationships of the new series are well described with QSAR and CoMFA models.

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 112-80-1 Product Details of 112-80-1.

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The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic, spectroscopic, and theoretical assessments of solvent structures and their interactions with reaction intermediates. Formula: https://www.ambeed.com/products/112-62-9.html.

Quinuclidin-3-yl 2-cyclopentyl-2-hydroxy-2-phenylacetate, a more effective the muscarinic receptor antagonist, was synthesised and its crystal structure was first elucidated by X-ray crystallography.

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Researchers are common within chemical engineering and are often tasked with creating and developing new chemical techniques, frequently combining other advanced and emerging scientific areas. In a document, author is Prickaerts, Jos, introducing its new discovery. Safety of 7-Aminocephalosporanic acid.

EVP-6124, (R)-7-chloro-N-quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, is a novel partial agonist of alpha 7 neuronal nicotinic acetylcholine receptors (nAChRs) that was evaluated here in vitro and in vivo. In binding and functional experiments, EVP-6124 showed selectivity for alpha 7 nAChRs and did not activate or inhibit heteromeric alpha 4 beta 2 nAChRs. EVP-6124 had good brain penetration and an adequate exposure time. EVP-6124 (0.3 mg/kg, p.o.) significantly restored memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) in an object recognition task (ORT). Although donepezil at 0.1 mg/kg, p.o. or EVP-6124 at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory. In a natural forgetting test, an ORT with a 24 h retention time. EVP-6124 improved memory at 0.3 mg/kg, p.o. This improvement was blocked by the selective alpha 7 nAChR antagonist methyllycaconitine (0.3 mg/kg, i.p. or 10 mu g, i.c.v.). In co-application experiments of EVP-6124 with acetylcholine, sustained exposure to EVP-6124 in functional investigations in oocytes caused desensitization at concentrations greater than 3 nM, while lower concentrations (0.3-1 nM) caused an increase in the acetylcholine-evoked response. These actions were interpreted as representing a co-agonist activity of EVP-6124 with acetylcholine on alpha 7 nAChRs. The concentrations of EVP-6124 that resulted in physiological potentiation were consistent with the free drug concentrations in brain that improved memory performance in the ORT. These data suggest that the selective partial agonist EVP-6124 improves memory performance by potentiating the acetylcholine response of alpha 7 nAChRs and support new therapeutic strategies for the treatment of cognitive impairment. This article is part of a Special Issue entitled ‘Post-Traumatic Stress Disorder’. (C) 2011 Elsevier Ltd. All rights reserved.

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Chemical engineers work across a number of sectors, processes differ within each of these areas, and are directly involved in the design, development, creation and manufacturing process of chemical products and materials. Like 13419-61-9, Name is Sodium decane-1-sulfonate. In a document, author is Dolle, F, introducing its new discovery. Related Products of 13419-61-9.

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.

Related Products of 13419-61-9, Therefore, this conceptually novel strategy might open impressive avenues to establish green and sustainable chemistry platforms.In my other articles, you can also check out more blogs about 13419-61-9.

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You could be based in a university, combining chemical research with teaching; or in a public-sector research center, helping to ensure national healthcare provision keeps pace with new discoveries. Like 1889-67-4, Name is (2,3-Dimethylbutane-2,3-diyl)dibenzene. In a document, author is Primozic, Ines, introducing its new discovery. Computed Properties of https://www.ambeed.com/products/1889-67-4.html.

The orientations of chiral quinuclidin-3-ol esters and benzoylcholine in the active site of horse butyrylcholinesterase have been investigated by flexible ligand docking. Change of the esters’ acyl moiety as well as the substituent at the quinuclidinium nitrogen atom affected the activity and stereoselectivity of the biotransformations. Analysis of interactions in the active site revealed the most important binding patterns for enantiomers, which define their reactivity. Calculated Gibbs energies of binding obtained by molecular docking simulations were well correlated to the experimentally determined binding affinities of the investigated chiral esters. (doi: 10.5562/cca2060)

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 1889-67-4 Computed Properties of https://www.ambeed.com/products/1889-67-4.html.

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When developing chemical systems it’s of course important to gain a deep understanding of the chemical reaction process. In a document, author is Lopez-Rodriguez, ML, introducing its new discovery. HPLC of Formula: https://www.ambeed.com/products/3159-07-7.html.

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).

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.If you’re interested in learning more about 3159-07-7. The above is the message from the blog manager. HPLC of Formula: https://www.ambeed.com/products/3159-07-7.html.

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When developing chemical systems it’s of course important to gain a deep understanding of the chemical reaction process. In a document, author is Bosak, A, introducing its new discovery. SDS of cas: 2386-53-0.

The (R)- and (S)-enantiomers of quinuclidin-3-ol and quinuclidin-3-yl acetate as well as their quaternary N-methyl and N-benzyl derivatives were synthesized in order to study the stereo-selectivity of human erythrocyte acetylcholinesterase (EC 3.1.1.7) and plasma butyrylcholinesterase (EC 3.1.1.8). The compounds were tested as substrates and inhibitors of cholinesterases. Both cholinesterases hydrolyze the derivatives of quinuclidin-3-yl acetate with a preference for the (R)- over (S)-enantiomers. In contrast to the hydrolysis of the enantiomers of acetates, the inhibition of acetylcholinesterase and butyrylcholinesterase by the (R)- and (S)-enantiomers of quinuclidin-3-ol derivatives does not reveal enantiomeric preference of the enzymes. The (R)and (S)-acetates also act as nonstereoselective inhibitors of the enzyme-induced hydrolysis of acetylthiocholine. The best substrate is (R)-N-methyl-3-acetoxyquinuclidinium iodide with k(cat) = 1.5 x 10(6) min(-1) and k(cat) = 5.5 x 10(4) min(-1) for acetylcholinesterase and butyrylcholinesterase, respectively. The (R)- and (S)-N-benzylquinuclidinium derivatives are the most potent inhibitors of both enzymes.

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 2386-53-0 SDS of cas: 2386-53-0.

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Chemical engineers work across a number of sectors, processes differ within each of these areas, and are directly involved in the design, development, creation and manufacturing process of chemical products and materials. Like 31906-04-4, Name is 4-(4-Hydroxy-4-methylpentyl)cyclohex-3-enecarbaldehyde. In a document, author is Niphade, Navnath C., introducing its new discovery. HPLC of Formula: https://www.ambeed.com/products/31906-04-4.html.

The development of an efficient and economic one-pot process, in which the configuration of the chiral centers of the starting materials is retained, for the preparation of highly pure solifenacin succinate, an antimuscarinic agent, is presented in this communication. The earlier reported processes suffer from the drawbacks of racemization and low yields due to the use of strong base, higher temperatures, and longer reaction times. The present work circumvents these issues by activating (3R)-quinuclidin-3-ol into a mixed active carbonate derivative by treating it with bis(4-nitrophenyl)carbonate. The subsequent reaction of the active carbonate with an enantiomerically pure amine without using any base at ambient temperature provided enantiomerically pure solifenacin with an overall yield of 90%.

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Chemical research careers are more diverse than they might first appear, as there are many different reasons to conduct research and many possible environments. Like 68131-04-4, Name is Sodium bicyclo[2.2.1]hept-5-ene-2,3-dicarboxylate. In a document, author is Ugawa, T, introducing its new discovery. Related Products of 68131-04-4.

1 The aim of this study was to establish an experimental model of the escape phenomenon, in which plasma cholesterol, initially reduced by a 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase inhibitor such as pravastatin, increases again on long-term administration. We also evaluated the efficacy of YM-53601 ((E)-2-[2-fluoro-2- (quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a squalene synthase inhibitor, in this model. 2 Pravastatin inhibited cholesterol biosynthesis in hamster primary hepatocytes (IC50, 14 nM). After pre-treatment with pravastatin, in contrast, almost no effect on cholesterol biosynthesis was seen. 3 In hamsters fed a high fat diet, 3 mg kg(-1) pravastatin for 9 days decreased plasma non-HDL cholesterol (total cholesterol-high density lipoprotein cholesterol) (P<0.01), but this effect was lost between 17 and 27 days of treatment, accompanied by an increase in HMG-CoA reductase activity. No such increase in plasma non-HDL cholesterol was seen with YM-53601 at 30 mg kg(-1) after 9 (P<0.001), 17 (P<0.01) or 27 (P<0.001) days of treatment. Replacement of pravastatin with YM-53601 caused a decrease in plasma non-HDL cholesterol by 53% (P<0.001) and in HMG-CoA reductase activity. 4 This animal model thus satisfactorily replicates the escape phenomenon observed in humans and may therefore be useful in evaluation of lipid-lowering agents, specifically comparison of HMG-CoA reductase inhibitors. Further, YM-53601 may be useful in the treatment of hypercholesterolemia without induction of the escape phenomenon. 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.Interested yet? Keep reading other articles of 68131-04-4, you can contact me at any time and look forward to more communication. Related Products of 68131-04-4.

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Computed Properties of https://www.ambeed.com/products/5324-84-5.html, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 5324-84-5, Name is Sodium octane-1-sulfonate, SMILES is CCCCCCCCS(=O)([O-])=O.[Na+], belongs to quinuclidine compound. In a article, author is Tudosie, Mihail S., introduce new discover of the category.

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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