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YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki 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 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.html" class="link-product" target="_blank">Oxybutynin (HY-B0267), and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats[1].
| [IC 50]
mAChR3: 15 nM (Ki); mAChR1: 28 nM (Ki); mAChR2: 260 nM (Ki) | [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. DOI:10.1248/cpb.46.1274 |
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