产品
编 号：F273261
分子式：C27H32ClN3O2
分子量：466.01
分子式：C27H32ClN3O2
分子量：466.01
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 214558-72-2
产品详情
生物活性：
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.
体内研究：
YM-58790 (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice. YM-58790 (6.0 mg/kg; i.v.) shows poor M1 and M2 antagonism effect in vivo on McN-A343-induced pressor in pithed rats, but displays potent efficacy on M3 antagonism with an ED30 value of 0.36 mg/kg (i.v.) and an ID50 value of 2.4 mg/kg (i.v.). YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction, similar to Oxybutynin (HY-B0267), and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats.
体外研究：
YM-58790 (compound 18b) (0-1 μM) 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.
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.
体内研究：
YM-58790 (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice. YM-58790 (6.0 mg/kg; i.v.) shows poor M1 and M2 antagonism effect in vivo on McN-A343-induced pressor in pithed rats, but displays potent efficacy on M3 antagonism with an ED30 value of 0.36 mg/kg (i.v.) and an ID50 value of 2.4 mg/kg (i.v.). YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction, similar to Oxybutynin (HY-B0267), and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats.
体外研究：
YM-58790 (compound 18b) (0-1 μM) 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备