Neurotransmitter transporters are membrane proteins that serve as key regulators of extracellular neurotransmitter concentrations and have been long viewed as important targets for drug development by the pharmaceutical industry. Although many cellular signaling systems are known to modulate transport activity, much less is known about how transporters communicate with and are regulated by the various components of the lipid sea in which they reside. Variations in lipid content clearly affect the activity of a variety of transport systems, and with advances in techniques for lipid analysis and a clearer vision of carrier structure, this area of research appears poised for major advances.