| Identification | Back Directory | [Name]
Zamifenacinfumarate | [CAS]
127308-98-9 | [Synonyms]
UK-76654 fumarate
Zamifenacinfumarate
(3R)-1-[2-(1-,3-Benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)piperidinefumarate | [Molecular Formula]
C27H29NO3.C4H4O4 | [MDL Number]
MFCD09263617 | [MOL File]
127308-98-9.mol | [Molecular Weight]
531.602 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
Soluble to 100 mM in DMSO and to 25 mM in ethanol | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Zamifenacin Fumarate is a selective antagonist of mAChR M3 (M3 muscarinic receptor). | [Biological Activity]
Selective M 3 muscarinic receptor antagonist (pK i values are 8.52, 7.93, 7.90 and 7.78 for M 3 , M 2 , M 1 and M 4 receptors respectively). Displays higher affinity at ileal M 3 receptors (pK i = 9.3) compared to oesophageal and tracheal M 3 receptors (pK i values are 8.8 and 8.2 respectively). In vivo, inhibits gastrointestinal motility in the absence of cardiovascular effects. | [in vivo]
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]. | Animal Model: | Male CDl mice (mean weight 23 g)[2] | | Dosage: | 5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous administration and oral administration | | Result: | Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (1.1 h). |
| Animal Model: | Male and female CD rats (mean weight 210 g)[2] | | Dosage: | 5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous administration and oral administration | | Result: | Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h). |
| Animal Model: | Male and two female beagle dogs (13-16 kg)[2] | | Dosage: | 1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous administration and oral administration | | Result: | Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h). |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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