The delta opioid receptor has become increasingly relevant to the development of analgesics since its discovery only a few decades past. The endogenous antinociceptive properties of the δOR in conjunction with the potential for δOR ligands to circumvent classical μ-opioid side effects and tolerance make the δOR a provocative alternative to current μOR-specific strategies. This chapter explores the clinical potential of δOR-mediated analgesia and discusses novel biochemical strategies for targeting the δOR. Finally, we evaluate the use of δOR ligands as co-therapies with new and classical analgesics. A greater understanding of δOR function and pharmacology will ultimately contribute to the development of innovative new strategies for the pharmacological management of pain.