Opiates derived from the opium poppy, Papaver somniferum, have been used in for millenia for their anti-diarrheal, analgesic and euphoric properties. More recently, endogenous peptides, enkephalins, dynorphins, and endorphins, were found to bind to the same sites as opiate alkaloids. The receptors for the classical opioids are three related GPCRs, delta, kappa, and mu (also known as OP1, OP2 and OP3, resepctively), that activate Gi/o to reduce intracellular cAMP levels. Although most clinically used opioids function by activation of the µ opioid receptor, agonits of spinal delta opioid receptors have antinociceptive activity that is independent of µ. In addition, activation of delta increases locomotor activity, inhibits gastrointestinal motility, and decreases respiratory frequency (Dhawan et al., 1996). Agonists for delta opioid receptors also exhibit antidepressant-like activity in animal models (Broom et al., 2002). Chemicon's delta membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of agonists and antagonists at delta. The membrane preparations exhibit a Kd of 1.12 nM for [3H]-DADLE. With 0.9 nM [3H]-DADLE, 10 µg/well delta Membrane Prep typically yields greater than 4-fold signal-to-background ratio.
Application: Radioligand binding assay and GTPgammaS
Biochem Physiol Actions: Target Sub-Family: Opioid
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