66164-07-6

Off-White Solid

A metabolite of Loperamide; a new and improved PET radiotracer for imaging P-gp function

Loperamide is an opiate which potently and selectively activates μ opioid receptors (Ki = 0.16 nM) exclusively in the periphery. N-Desmethyl-loperamide (dLop) is a major metabolite of loperamide. Like loperamide, dLop is a substrate of the ATP-dependent efflux transporter, P-glycoprotein. As a result, both the parent compound and the metabolite display restricted passage through the blood-brain barrier. dLop in biological samples can be analyzed by a variety of methods.

ChEBI: A monocarboxylic acid amide that is the methylamide of 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylbutanoic acid.