An active metabolite of alvimopan
货号:ajcx25400
CAS:170098-43-8
分子式:C23H29NO3·HCl
分子量：403.9
溶解度:DMSO: soluble,Methanol: soluble
纯度：98%
存储：Store at -20°C
库存：现货

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 (K_i= 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (K_is = 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)