Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner.In an article, author is Naito, R, once mentioned the application of 765-70-8, Name is 3-Methylcyclopentane-1,2-dione, molecular formula is C6H8O2, molecular weight is 112.13, MDL number is MFCD00001417, category is quinuclidines. Now introduce a scientific discovery about this category, Recommanded Product: 3-Methylcyclopentane-1,2-dione.
Selective muscarinic antagonists. II. Synthesis and antimuscarinic properties of biphenylylcarbamate derivatives
A novel series of biphenylylcarbamate derivatives were synthesized and evaluated for binding to M-1, M-2 and M-3 receptors and for antimuscarinic activities. Receptor binding assays indicated that biphenyl-2-ylcarbamate derivatives had high affinities for M-1 and M-3 receptors and good selectivities for M-3 receptor over M-2 receptor, indicating that the biphenyl-2-yl group is a novel hydrophobic replacement for the benzhydryl group in the muscarinic antagonist field. In this series, quinuclidin-1-yl biphenyl-2-ylcarbamate monohydrochloride (81, YM-46303) exhibited the highest affinities for M-1 and M-3 receptors, and selectivity for M-3 over M-2 receptor. Compared to oxybutynin, YM-46303 showed approximately ten times higher inhibitory activity on bladder pressure in reflexly-evoked rhythmic contraction, and about 5-fold greater selectivity for urinary bladder contraction against salivary secretion in rats. Moreover, selective antagonistic activity was also observed in vitro. Further evaluation of antimuscarinic effects on bradycardia and presser in pithed rats, and on tremor in mice, showed that YM-46303 can be useful for the treatment of urinary urge incontinence as a bladder-selective M-3 antagonist with potent activities and fewer side effects.
The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.Interested yet? Keep reading other articles of 765-70-8, you can contact me at any time and look forward to more communication. Recommanded Product: 3-Methylcyclopentane-1,2-dione.
Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider