YM-58790 free base 

YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with K_i values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats^[1].

YM-58790 free base (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

429.55

C₂₇H₃₁N₃O₂

168830-70-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Naito R, et al. Selective muscarinic antagonists. I. Synthesis and antimuscarinic properties of 4-piperidyl benzhydrylcarbamate derivatives. Chem Pharm Bull (Tokyo). 1998 Aug;46(8):1274-85.  [Content Brief]