Darifenacin (hydrobromide)

Darifenacin is an antagonist of M3 muscarinic acetylcholine receptors (mAChRs, Ki = 0.76 nM). 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.Formal Name: 1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-alpha,alpha-diphenyl-3-pyrrolidineacetamide, monohydrobromide. CAS Number: 133099-07-7. Synonyms: UK 88525-04. Molecular Formula: C28H30N2O2 . HBr. Formula Weight: 507.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 2 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 205, 287 nm. SMILES: NC(C(C1=CC=CC=C1)(C2=CC=CC=C2)[C@H]3CN(CCC4=CC=C(OCC5)C5=C4)CC3)=O.Br. InChi Code: InChI=1S/C28H30N2O2.BrH/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26,/h1-12,19,25H,13-18,20H2,(H2,29,31),1H/t25-,/m1./s1. InChi Key: UQAVIASOPREUIT-VQIWEWKSSA-N.