alvimopan

Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.

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

Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active, and reversible μ-opioid receptor antagonist with an IC50 of 1.7 nM. Highly selective for the μ-opioid receptor (Ki = 0.47 nM) over κ- and δ-opioid receptors (Kis = 100 and 12 nM, respectively), Alvimopan dihydrate can be used for research on postoperative ileus [1] [2] [3].

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.