产品属性:
产品名称 | ADL 08-0011 (hydrochloride) |
规格 | 1 mg、5 mg、10 mg |
货号 | EY-01Y16173 |
Cas No.: 170098-43-8
别名: N/A
化学名: N/A
分子式: C23H29NO3·HCl
分子量: 403.9
溶解度: DMSO: soluble,Methanol: soluble
储存条件: -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan .1 It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverses loperamide-induced delayed gastric emptying in a rat model of castor oil-induced diarrhea.21.Beattie, D.T., Cheruvu, M., Mai, N., et al.The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, alvimopan, ADL 08-0011 and methylnaltrexoneNaunyn Schmiedebergs Arch. Pharmacol.375(3)205-220(2007)
2.Armstrong, S.R., Campbell, C.B., Richardson, C.L., et al.The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activityNaunyn Schmiedebergs Arch Pharmacol.386(6)471-478(2013)
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