Category: 502-49-8

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 502-49-8, Name is Cyclooctanone, SMILES is O=C1CCCCCCC1, in an article , author is Tang, Cuyue, once mentioned of 502-49-8, Category: quinuclidines.

Neuropharmacokinetics of two investigational compounds in rats: Divergent temporal profiles in the brain and cerebrospinal fluid

Two investigational compounds (FRM-1, (R)-7-fluoro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and FRM-2, (R)-7-cyano-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide) resided in rat brain longer than in systemic circulation. In Caco-2 directional transport studies, they both showed good intrinsic passive permeability but differed significantly in efflux susceptibility (efflux ratio of <2 and similar to 7, respectively), largely attributed to P-glycoprotein (P-gp). Capitalizing on these interesting properties, we investigated how cerebrospinal fluid (CSF) concentration (C-CSF) would be shaped by unbound plasma concentration (C-u,C-p) and unbound brain concentration (C-u,C-b) in disequilibrium conditions and at steady state. Following subcutaneous administration, FRM-1 C-CSF largely followed C-u,C-p initially and leveled between C-u,C-p and C-u,C-b. However, it gradually approached C-u,C-b and became lower than, but parallel to C-u,C-b at the terminal phase. In contrast, FRM-2 C-CSF temporal profile mostly paralleled the C-u,C-p but was at a much lower level. Upon intravenous infusion to steady state, FRM-1 C-CSF and C-u,C-b were similar, accounting for 61% and 69% of the Cu, indicating a case of largely passive diffusion-governed brain penetration where C-CSF served as a good surrogate for C-u,C-b. On the contrary, FRM-2 C-CSF and C-u,C-b were remarkably lower than C-u,C-p, (17% and 8% of C-u,C-p respectively), suggesting that FRM-2 brain penetration was severely impaired by P-gp-mediated efflux and C-CSF underestimated this impact. A semi-physiologically based pharmacokinetic (PBPK) model was constructed that adequately described the temporal profiles of the compounds in the plasma, brain and CSF. Our work provided some insight into the relative importance of blood-brain barrier (BBB) and blood-CSF barrier (BCSFB) in modulating CCSF. (C) 2014 Elsevier Inc. All rights reserved. Interested yet? Read on for other articles about 502-49-8, you can contact me at any time and look forward to more communication. Category: quinuclidines.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 502-49-8, Name is Cyclooctanone, SMILES is O=C1CCCCCCC1, in an article , author is Primozic, Ines, once mentioned of 502-49-8, Product Details of 502-49-8.

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.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 502-49-8, you can contact me at any time and look forward to more communication. Product Details of 502-49-8.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Related Products of 502-49-8, 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. 502-49-8, Name is Cyclooctanone, SMILES is O=C1CCCCCCC1, belongs to quinuclidines compound. In a article, author is Prickaerts, Jos, introduce new discover of the category.

EVP-6124, a novel and selective alpha 7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of alpha 7 nicotinic acetylcholine receptors

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.

Related Products of 502-49-8, 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 502-49-8.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

502-49-8, Name is Cyclooctanone, molecular formula is C8H14O, belongs to quinuclidines compound, is a common compound. In a patnet, author is Lopez-Rodriguez, ML, once mentioned the new application about 502-49-8, HPLC of Formula: C8H14O.

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).

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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider