desmethyl-loperamide

Desmethyl-loperamide is a major active metabolite of the antidiarrheal drug loperamide. It is a synthetic phenylpiperidine opioid that acts as a peripherally selective μ-opioid receptor agonist, similar to its parent compound. Both desmethyl-loperamide and loperamide are substrates of the ATP-dependent efflux transporter P-glycoprotein, which restricts their passage through the blood-brain barrier, limiting central nervous system effects. This metabolite retains activity at peripheral μ-opioid receptors to reduce gastrointestinal motility and fluid secretion, contributing to antidiarrheal effects. It has also been used as a PET radiotracer for imaging P-glycoprotein function due to its transport properties.

Other names

N-Desmethyl LoperamidN-Desmethyl LoperamideDesmethylloperamide D5Desmethyl loperamide HCl