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產品描述： Darifenacin is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome. |
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靶點：
AChR |
體內研究：
Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB). |
參考文獻：
1.Hegde SS, et al. Br J Pharmacol, 1997, 120(8), 1409-1418. 2.Haab F, et al. Eur Urol, 2004, 45(4), 420-429. 3.Miller DW, et al. Neurourol Urodyn, 2011, 30(8), 1633-1638. 4.Iijima K, et al. Eur Urol, 2007, 52(3), 842-847. |
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溶解性：
Ethanol:<1 mg/mL H2O:<1 mg/mL DMSO:93 mg/mL (184 mM) |
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保存條件：
2-8℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
1.971 ml |
9.853 ml |
19.706 ml |
| 5 mM |
0.394 ml |
1.971 ml |
3.941 ml |
| 10 mM |
0.197 ml |
0.985 ml |
1.971 ml |
| 50 mM |
0.039 ml |
0.197 ml |
0.394 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京