An internal standard for the quantification of darifenacin
货号:ajcx24220
CAS:1189701-43-6
分子式:C28H26D4N2O2
分子量：430.6
溶解度:Acetonitrile: soluble,DMSO: soluble
纯度：98%
存储：Store at -20°C
库存：现货

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; K_i= 0.76 nM).¹It is selective for M₃over M₁, M₂, M₄, and M₅mAChRs (K_is = 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)