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^[1]. 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^[1]. In Vivo: YM-58790 (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice^[1].
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.)^[1].
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^[1].