For research use only. Not for therapeutic Use.
Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].
Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg)[2].
Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg)[2].
| Catalog Number | M111754 |
| CAS Number | 127308-98-9 |
| Synonyms | (3R)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine;(E)-but-2-enedioic acid |
| Molecular Formula | C31H33NO7 |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | PMHKTAIGYOVZEZ-ZHWJIHCSSA-N |
| SMILES | C1CC(CN(C1)CCC2=CC3=C(C=C2)OCO3)OC(C4=CC=CC=C4)C5=CC=CC=C5.C(=CC(=O)O)C(=O)O |
| Reference | [1]. Houghton LA, et al. Zamifenacin (UK-76, 654) a potent gut M3 selective muscarinic antagonist, reduces colonic motor activity in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1997 Jun;11(3):561-8. [2]. Beaumont KC, et al. Pharmacokinetics and metabolism of Zamifenacin in mouse, rat, dog and man. Xenobiotica. 1996 Apr;26(4):459-71. |
