214558-72-2

214558-72-2 structure

Name	YM-58790
Synonyms	Carbamic acid, N-(diphenylmethyl)-, 1-[[4-(methylamino)phenyl]methyl]-4-piperidinyl ester, hydrochloride (1:1) 1-[4-(Methylamino)benzyl]-4-piperidinyl (diphenylmethyl)carbamate hydrochloride (1:1)

Description	YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mAChR Signaling Pathways >> Neuronal Signaling >> mAChR Research Areas >> Others
Target	Ki: 15 nM (M3 muscarinic receptor)[1]
In Vitro	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].
In Vivo	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].
References	[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.