alvimopan

Alvimopan (LY 246736) 是一种选择性和竞争性 μ 阿片受体拮抗剂，IC50值为 1.7 nM。它存在于肌间和黏膜下神经元以及人体肠道固有层的免疫细胞中，可用于术后肠梗阻的研究。

Alvimopan dihydrate（ADL 8-2698 dihydrate）是一种有效的μ-阿片受体（μ-opioid receptor）可逆拮抗剂，具备口服活性，选择性强，IC50值为1.7 nM。其对μ-阿片受体的选择性（Ki=0.47 nM）远高于κ-（Ki=100 nM）和δ-阿片受体（Ki=12 nM），显示出在术后肠梗阻研究中的潜力。

Alvimopan monohydrate is a mu-opioid receptor antagonist that intended for the treatment of constipation in patients who take opiates for pain.

ADL-08-0011 is an metabolite of alvimopan.

ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. 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.