Zamifenacin (fumarate)

Zamifenacin is an antagonist of M3 muscarinic acetylcholine receptors (Ki = 10 nM for the human receptor). It is selective for M3 over M1, M2, M4, and M5 receptors in radioligand binding assays using cells expressing recombinant human receptors (Kis = 55, 153, 68, and 34 nM, respectively). Zamifenacin inhibits cholecystokinin-induced small bowel motility (ED50 = 0.9 mg/kg) but does not increase heart rate (ED150 = 80.0 mg/kg) in dogs.Formal Name: (3R)-1-[2-(1,3-benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)-piperidine, (2E)-2-butenedioate. CAS Number: 127308-98-9. Synonyms: UK 76654. Molecular Formula: C27H29NO3 . C4H4O4. Formula Weight: 531.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 50 mg/ml, Ethanol: 20 mg/ml. SMILES: OC(/C=C/C(O)=O)=O.C(C1=CC=CC=C1)(C2=CC=CC=C2)O[C@H]3CN(CCC3)CCC4=CC=C(OCO5)C5=C4. InChi Code: InChI=1S/C27H29NO3.C4H4O4/c1-3-8-22(9-4-1)27(23-10-5-2-6-11-23)31-24-12-7-16-28(19-24)17-15-21-13-14-25-26(18-21)30-20-29-25,5-3(6)1-2-4(7)8/h1-6,8-11,13-14,18,24,27H,7,12,15-17,19-20H2,1-2H,(H,5,6)(H,7,8)/b,2-1+/t24-,/m1./s1. InChi Key: PMHKTAIGYOVZEZ-ZHWJIHCSSA-N.