delta Opioid Receptor Antagonists Small Molecules and Peptides

The δ opioid receptor (also known as OP₁, DOP, DOR) is a member of the opioid family of G-protein-coupled receptors that also includes μ, κ and NOP receptors. In the CNS, δ opioid receptors are primarily distributed in the olfactory bulb, nucleus accumbens, caudate putamen and neocortex, with low-moderate levels present in the thalamus, hypothalamus and brainstem.

δ opioid receptors play a role in analgesia, motor integration, gastrointestinal motility, olfaction, respiration, cognitive function and mood driven behavior. The enkephalins are generally considered to be the preferred endogenous ligands. The human gene encoding the δ opioid receptor has been localized to chromosome 1 (1p36.1-p34.3).