Formulation: A solid
Formal Name: 1-[2-(2,3-dihydro-5-benzofuranyl)ethyl-1,1,2,2-d4]-α,α-diphenyl-3-pyrrolidineacetamide
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C28H26D4N2O2
Formula Weight: 430,6
Shelf life (days): 1460
CAS Number: 1189701-43-6
Notes: Darifenacin-d4 is intended for use as an internal standard for the quantification of darifenacin (Item No. 14424) by GC- or LC-MS. Darifenacin is an antagonist of M3 muscarinic acetylcholine receptors (mAChRs; Ki = 0.76 nM).{59910} It is selective for M3 over M1, M2, M4, and M5 mAChRs (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 M3 mAChRs, over isolated rabbit vas deferens and isolated guinea pig atria (pA2s = 7.9 and 7.48, respectively), which endogenously express M1 and M2 mAChRs, 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.
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