| 应用 |
YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
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.
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. |
