Category: 97-65-4

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, Like 97-65-4, Name is Propylenedicarboxylic acid. In a document, author is Ikeda, K, introducing its new discovery. Recommanded Product: Propylenedicarboxylic acid.

M-3 receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland

The antimuscarinic profile of the experimental drug solifenacin/YM905 [(+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate] for the treatment of overactive bladder was compared with the commonly prescribed agent oxybutynin. In radioligand binding assays, pK(i) values of solifenacin for M-1, M-2, and M-3 receptors were 7.6, 6.9, and 8.0, respectively. These values for oxybutynin were 8.6 (M-1), 7.7 (M-2), and 8.9 (M-3). Solifenacin and oxybutynin antagonized the contractile effect of carbachol (CCh) on isolated guinea pig urinary bladder smooth muscle (detrusor), displaying the negative logarithm of antagonist apparent affinity constant (pK(b) value) of 7.1 for solifenacin and 7.4 for oxybutynin. To study the tissue selectivity between bladders and salivary glands, guinea pig detrusor and mouse submandibular gland cells were stimulated with CCh and monitored for intracellular Ca2+, as determined by Fura 2 fluorescence. Ca2+ mobilization of detrusor cells was inhibited equipotently by solifenacin (pK(i)=8.4) and oxybutynin (pK(i)=8.6), whereas that of the gland cells was antagonized less potently by solifenacin (pK(b)=7.4) than by oxybutynin (pK(b)=8.8), although the M-3 subtype mediated both cell responses. In anesthetized rats, solifenacin (63-2100 nmol kg(-1) or 0.03-1 mg kg(-1)) dose-dependently inhibited CCh-stimulated increases in urinary bladder pressure, while its inhibitory effects on salivation and bradycardia were apparent only at a dose of 2100 nmol kg(-1). In contrast, oxybutynin within a dose range of 77-770 nmol kg(-1) (0.03-0.3 mg kg(-1)) inhibited responses of the bladder and salivary gland slightly more potently than that of the heart. In addition, inhibitory effects of darifenacin indicated a major role Of M-3 receptors in the bladder and salivary gland. Therefore, M-3 receptor antagonism by solifenacin could be bladder-selective. This selectivity remains to be elucidated and may provide new approaches to the pharmacotherapy of overactive bladder.

Enzymes are biological catalysts that produce large increases in reaction rates.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 97-65-4, Recommanded Product: Propylenedicarboxylic acid.

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

Synthetic Route of 97-65-4, 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. 97-65-4, Name is Propylenedicarboxylic acid, SMILES is O=C(O)C(CC(O)=O)=C, belongs to quinuclidines compound. In a article, author is Nomoto, F, introduce new discover of the category.

A practical chemoenzymatic process to access (R)-quinuclidin-3-ol on scale

(+/-)-3-Butyryloxyquinuclidinium butyrate 6 (2 M, 571 g/L), prepared from (+/-)-quinuclidin-3-ol 1 and butyric anhydride, undergoes enantioselective hydrolysis by an Aspergillus melleus protease {1.0% (w/v)} in water in the presence of Ca(OH)(2) to keep the reaction at pH 7 and trap butyric acid that is introduced as part of (+/-)-6 and generated by the enzymatic hydrolysis. After a 24 h period, extraction with n-heptane provides (R)-quinuclidin-3-yl butyrate 5a, which, on methanolysis with Na2CO3, is converted into (R)-1, a common pharmacophore of neuromodulators acting on muscarinic receptors, in 96% ee and 42% overall yield from (+/-)-1. The unwanted antipode (S)-1, which is extracted into n-butanol and purified via its hydrochloride salt in 89% ee and 40% overall yield from (+/-)-1, can be racemized by the catalysis of Raney Co at 140degreesC under an atmosphere of H, (5 kg/cm(2)) to regenerate (+/-)-1 in 97% yield. (C) 2003 Elsevier Science Ltd. All rights reserved.

Synthetic Route of 97-65-4, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 97-65-4 is helpful to your research.

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

Synthetic Route of 97-65-4, 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. 97-65-4, Name is Propylenedicarboxylic acid, SMILES is O=C(O)C(CC(O)=O)=C, belongs to quinuclidines compound. In a article, author is HACKSELL, U, introduce new discover of the category.

QUINUCLIDIN-2-ENE – BASED MUSCARINIC ANTAGONISTS

A series of achiral 3-heteroaryl substituted quinuclidin-2-ene derivatives and related compounds have been synthesized by facile methods. The compounds were evaluated for muscarinic and antimuscarinic properties in receptor binding studies using (-)-[H-3]-QNB as the radioligand and ina functional assay using isolated guinea pig urinary bladder. 3-(2-Benzofuranyl)-quinuclidin-2-ene (15) displayed the highest M(1)-receptor affinity in the present series (K-i = 9.6 nM).

Synthetic Route of 97-65-4, 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 97-65-4.

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

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 97-65-4, Name is Propylenedicarboxylic acid, molecular formula is , belongs to quinuclidines compound. In a document, author is Naito, R, Recommanded Product: Propylenedicarboxylic acid.

Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists

In the course of continuing efforts to develop potent and bladder-selective muscarinic M-3 receptor antagonists, quinuclidin-3-yl 1-aryl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives and related compounds were designed as conformationally restricted analogues of quinuclidin-3-yl benzhydrylcarbamate (8). Binding assays with rat muscarinic receptor subtypes revealed that the quinuclidin-3-yl 1-aryl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives showed high affinities for the M3 receptor, and selectivity for the M3 receptor over the M-2 receptor. Of these derivatives, (+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monohydrochloride (9b) exhibited almost the same inhibitory activity against bladder contraction to that of oxybutynin (1), and more than 10-fold selectivity for bladder contraction versus salivary secretion, demonstrating that 9b may be useful for the treatment of symptoms associated with overactive bladder without having side effects such as dry mouth.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 97-65-4, in my other articles. Recommanded Product: Propylenedicarboxylic acid.

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