| 规格: | 98% |
| 分子量: | 430.6 |
| 包装 | 价格(元) |
| 500ug | 电议 |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
Background:
Darifenacin-d4is intended for use as an internal standard for the quantification of darifenacin by GC- or LC-MS. Darifenacin is an antagonist of M3muscarinic acetylcholine receptors (mAChRs; Ki= 0.76 nM).1It is selective for M3over M1, M2, M4, and M5mAChRs (Kis = 7.08, 44.67, 45.71, and 9.33 nM, respectively). Darifenacin selectively inhibits contractions in isolated guinea pig ileum, bladder, and trachea (pA2s = 9.44, 8.66, and 8.7, respectively), tissues that endogenously express high levels of M3mAChRs, over isolated rabbit vas deferens and isolated guinea pig atria (pA2s = 7.9 and 7.48, respectively), which endogenously express M1and M2mAChRs, respectively. It inhibits micturition pressure (ED50= 0.089 mg/kg, i.v.), as well as micturition interval and volume in rats. Formulations containing darifenacin have been used in the treatment of overactive bladder.
1.Wallis, R.M., and Napier, C.M.Muscarinic antagonists in development for disorders of smooth muscle functionLife Sci.64(6-7)395-401(1999)
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