∂-Opioid Receptor Antibodies
Activation of the δ-opioid receptor (delta-opioid receptor, DOP) results in analgesic, antidepressant and anxiolytic effects in a number of animal models. Whereas high-efficacy DOP agonists such as SNC80 also produce convulsions, low-efficacy DOP agonists such ARD-353 or ARM100390 do not. The cyclic enkephalin analog DPDPE (H-Tyr-c[D-Pen-Gly-Phe-D-Pen]) is used as selective δ-agonist for in vitro studies. DOP desensitization, trafficking and signaling are regulated by phosphorylation of carboxyl-terminal threonine361 (pT361-DOP) and serine363 (pS363-DOP) residues. S363 is the primary site in a hierarchical phosphorylation cascade. Both T361 and S363 can be phosphorylated by GRK2 and GRK3 but not by PKC. This nomenclature refers to the human DOP. The sequence of this phosphorylation motif is highly conserved in mice, rats and humans. For more information on δ-opioid receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Gendron L, Cahill CM, von Zastrow M, Schiller PW, Pineyro G. Molecular Pharmacology of δ-Opioid Receptors. Pharmacol Rev. 2016 Jul;68(3):631-700. doi: 10.1124/pr.114.008979. Review. PubMed PMID: 27343248; PubMed Central PMCID: PMC4931872.