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, µ kappa and delta that activate Gi/o to reduce intracellular cAMP levels. Most clinically used opioids function by activation of the µ opioid receptor (Dhawan et al., 1996). Chemicon's µ opioid receptor 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 µ opioid receptor interactions with its ligands. The membrane preparations exhibit an EC50 of 1.6nM for DAMGO in a GTPgammaS binding assay.
Application: GTPgammaS Binding and Radioligand Binding Assay.
Biochem Physiol Actions: Target Sub-Family: Opioid
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