ileus

AS-35 is an orally effective, potent, and selective antagonist of leukotrienes, antagonizing LTC4-, LTD4-, and LTE4-induced ileum contractions with IC50 values of 8 nM, 4 nM, and 3 nM, respectively. It exhibits antiallergic activities.

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.

TU-100 is frequently used in the treatment of chronic gastrointestinal disorders, and it is commonly applied to alleviate symptoms such as abdominal pain, bloating, Crohn’s disease, irritable bowel syndrome, adhesive intestinal obstruction, and paralytic ileus. Additionally, TU-100 can improve gastrointestinal motility abnormalities in patients with grade B liver impairment after hepatectomy and reduce serum CRP levels.

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].