Alvimopan dihydrate

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Chemical Structure| 170098-38-1 同义名 : 爱维莫潘 ;LY 246736 dihydrate; ADL 8-2698 dihydrate; Alvimopan hydrate; Entereg; Alvimopan(dihydrate)
CAS号 : 170098-38-1
货号 : A397796
分子式 : C25H36N2O6
纯度 : 99%
分子量 : 460.56
MDL号 : MFCD00927248
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(75.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Alvimopan, a peripherally acting mu-opioid receptor antagonist, is a novel agent for the treatment of postoperative ileus[3]. Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 nM[4]. Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of 113Sn-labelled microspheres produced by morphine in rats. Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[5]. Mesenteric afferent fibres are markedly stimulated by mu-opioid receptor agonists, an effect blocked by alvimopan, which may contribute to the gastrointestinal reflex and behavioural responses to opiate treatment or abuse[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.86mL

2.17mL

1.09mL

21.71mL

4.34mL

2.17mL
参考文献

[1]Fukuda H, Suenaga K, et al. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70.

[2]Cassel JA, Daubert JD, et al. [(3)H] Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36.

[3]Bream-Rouwenhorst HR, Cantrell MA. Alvimopan for postoperative ileus. Am J Health Syst Pharm. 2009 Jul 15;66(14):1267-77

[4]Le Bourdonnec B, Barker WM, Belanger S, Wiant DD, Conway-James NC, Cassel JA, O'Neill TJ, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12

[5]Fukuda H, Suenaga K, Tsuchida D, Mantyh CR, Pappas TN, Hicks GA, Dehaven-Hudkins DL, Takahashi T. The selective mu opioid receptor antagonist, alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res. 2006 Aug 2;1102(1):63-70

[6]Grundy D, Booth CE, Winchester W, Hicks GA. Peripheral opiate action on afferent fibres supplying the rat intestine. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:29-37