YM-58790是一种有效的M3muscarinic受体拮抗剂，Ki值为15nM。
CAS：214558-72-2
分子式：C27H32ClN3O2
分子量：466.01
纯度：98%
存储：Store at -20°C

Background:

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[1].

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[1].

[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.