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214558-72-2

中文名稱 214558-72-2
英文名稱 YM-58790
CAS 214558-72-2
分子式 C27H32ClN3O2
分子量 466.02
MOL 文件 214558-72-2.mol
214558-72-2 結(jié)構(gòu)式 214558-72-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T13372
英文別名
YM-58790

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色Light yellow to yellow

常見問題列表

生物活性
YM-58790 是一種有效的 M3 muscarinic 受體拮抗劑,Ki 值為 15 nM。
靶點

Ki: 15 nM (M3 muscarinic receptor)

體外研究

YM-58790 shows potent inhibitory effect on urinary bladder contraction, but has little effect on bradycardia. YM-58790 exhibits selective antagonism between urinary bladder contraction and salivary secretion in vitro.

體內(nèi)研究

YM-58790 (3 mg/kg, i.v.) does not inhibit oxotremorine-induced tremor in mice. The effect of YM-58790 on McN-A343-induced pressor in pithed rats, as an indication of M1 antagonism in vivo, is much less potent than bladder contraction. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction, similar to oxybutynin, and has appr ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats.

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