No longer considered a static, impenetrable barrier, the dynamic regulatory functions of the blood-brain barrier (BBB) have become increasingly apparent. This is particularly evident for the transport of peptides across the BBB. Interactions of peptides with the endothelial cells composing the BBB could lead to endocytosis and eventually transcytosis of peptides. It is helpful to understand pertinent characteristics of the BBB, the circumventricular organs (CVOs), and choroid plexuses. Here we describe the methods used for measurement of the passage of peptides across the BBB, illustrate the types of interactions of peptides with the BBB, and summarize current results with the BBB penetration of feeding-related peptides.