YM-58790

YM-58790 is a potent antagonist of mAChR . YM-58790 binds M1 , M2 , M3 with K i 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 ED 30 value of 0.36 mg/kg (i.v.) and an ID 50 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 , and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:mAChR3 15 nM (Ki) mAChR1 28 nM (Ki) mAChR2 260 nM (Ki)

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