Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 10160-87-9, Name is 3,3-Diethoxyprop-1-yne, molecular formula is C7H12O2, belongs to quinuclidines compound, is a common compound. In a patnet, author is Naito, R, once mentioned the new application about 10160-87-9, SDS of cas: 10160-87-9.
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.
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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider