Neuropeptide-membrane interactions are poorly understood, thus fluorescent neuropeptide probes may reveal new information about membrane interaction mechanisms. The addition of fluorescent labels to glycosylated endorphin analogs that demonstrate d-selective opioid activity is being pursued, in order to probe elements controlling neuropeptide interactions with membranes, especially transport across the blood brain barrier (BBB). The striking BBB penetration of these glycopeptides is attributed to adsorption-mediated endocytosis, rather than more commonly engineered drug delivery mechanisms like lipophilicity and diffusion. Measured BBB transport rates indicate significant amphipathic character, which is further supported by helical conformations evident from NMR and NOE-directed Monte Carlo calculations. Progress in fluorescent glycopeptide syntheses and in vitro fluorescence microscopy studies will be described.