| 规格: | 98% |
| 分子量: | 403.9 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
Background:
ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan .1It is produced from alvimopanviaamide 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.2
1.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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