Asimadoline (AMD)

Asimadoline (EMD-61753) is a drug which acts as a peripherally selective κ-opioid agonist. Because of its poor ability to cross the blood–brain barrier, asimadoline lacks the psychotomimetic effects of centrally acting kappa agonists, and consequently has more potential for medical use, and has been researched as a possible treatment for irritable bowel syndrome, with reasonable efficacy seen in clinical trials. Asimadoline is a potent κ-opioid receptor agonist with a diaryl acetamide structure. It acts as a complete agonist in in vitro assay. Asimadoline reduced sensation in response to colonic distension at subnoxious pressures in healthy volunteers and in IBS patients without alteration of colonic compliance. Asimadoline reduced satiation and enhanced the postprandial gastric volume (in female volunteers). However, there were no significant effects on gastrointestinal transit, colonic compliance, fasting or postprandial colonic tone.