∂-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:

Mann A, Liebetrau S, Klima M, Dasgupta P, Massotte D, Schulz S. Agonist-induced phosphorylation bar code and differential post-activation signaling of the delta opioid receptor revealed by phosphosite-specific antibodies. Sci Rep. 2020 May 22;10(1):8585. doi: 10.1038/s41598-020-65589-7. PMID: 32444688

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.