الصفحة الرئيسية>>Signaling Pathways>> Neuroscience>> Behavioral Neuroscience>>ADL 08-0011 (hydrochloride)

ADL 08-0011 (hydrochloride)

رقم الكتالوجGC49216

An active metabolite of alvimopan

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ADL 08-0011 (hydrochloride) التركيب الكيميائي

Cas No.: 170098-43-8

الحجم السعر المخزون الكميّة
1 mg
170٫00
متوفر
5 mg
805٫00
متوفر
10 mg
1526٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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

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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