产品说明书

	同义名 :	阿尔维莫潘 ;LY 246736;ADL 8-2698;Alvimopan. trade name Entereg.;HSDB 7704
	CAS号 :	156053-89-3
	货号 :	A114778
	分子式 :	C25H32N2O4
	纯度 :	99+%
	分子量 :	424.533
	MDL号 :	MFCD09838268
	存储条件：	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Alvimopan is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM[3]. Alvimopan has a greater affinity for the mu-receptor than the kappa- or sigma-opioid receptors (Ki = 0.77 nM). It has limited systemic bioavailability and higher affinity for the mu-opioid receptor than naloxone (Ki = 3.7 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 behavioral responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[5]. Alvimopan showed significant advantages over placebo in restoring gastro-intestinal function, and reduced time to discharge following major abdominal surgery, with acceptable side effects[6]. Alvimopan significantly reduced the incidence of ileus and NGT (nasogastric tube) placement following RC(radical cystectomy). NGT placement was associated with an increased need for reoperation for bowel complications in the setting of alvimopan[7].

临床研究
NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02109640	Postoperative Pain ... 展开 >> Postoperative Nausea and Vomiting 收起 <<	Phase 3	Completed	-	United Kingdom ... 展开 >> Western General Hospital Edinburgh, United Kingdom, EH4 2XU 收起 <<
NCT02109640	-		Completed	-	-
NCT00388479	Ileus	Phase 3	Completed	-	United States, Pennsylvania ... 展开 >> Various Exton, Pennsylvania, United States, 19341 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.36mL 0.47mL 0.24mL	11.78mL 2.36mL 1.18mL	23.56mL 4.71mL 2.36mL

参考文献

[1]Viscusi ER, Goldstein S, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc. 2006 Jan;20(1):64-70. Epub 2005 Dec 7. Erratum in: Surg Endosc. 2006 Mar;20(3):537. [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]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 [4]Neary P, Delaney CP. Alvimopan. Expert Opin Investig Drugs. 2005 Apr;14(4):479-88 [5]Greenwood-Van Meerveld B, Gardner CJ, Little PJ, Hicks GA, Dehaven-Hudkins DL. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53 [6]Tan EK, Cornish J, Darzi AW, Tekkis PP. Meta-analysis: Alvimopan vs. placebo in the treatment of post-operative ileus. Aliment Pharmacol Ther. 2007 Jan 1;25(1):47-57 [7]Packiam VT, Agrawal VA, Pariser JJ, Cohen AJ, Nottingham CU, Pearce SM, Smith ND, Steinberg GD. Redefining the implications of nasogastric tube placement following radical cystectomy in the alvimopan era. World J Urol. 2017 Apr;35(4):625-631