| Identification | Back Directory | [Name]
Alvimopan metabolite (ADL08-0011),hydrochloride salt | [CAS]
170098-43-8 | [Synonyms]
Alvimopan Impurity 21
ADL 08-0011 (hydrochloride)
Alvimopan Metabolite 1 (ADL 08-0011) HCl
Alvimopan metabolite (ADL08-0011),hydrochloride salt | [Molecular Formula]
C23H30ClNO3 | [MOL File]
170098-43-8.mol | [Molecular Weight]
403.95 |
| Hazard Information | Back Directory | [Uses]
Alvimopan metabolite hydrochloride is a peripherally restricted Opioid Receptor antagonist that inhibits the amplitude of electrically evoked contractions and spontaneous mechanical activity in guinea pig ileum[1]. | [Biological Activity]
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.2 | [storage]
-20°C | [References]
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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