Description
Introduction: OPRD1 is a G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. It inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. It plays a role in the perception of pain and in opiate-mediated analgesia. It also plays a role in developing analgesic tolerance to morphine.
Description: Human OPRD1 ACTOne is a HEK293-CNG cell line that expresses recombinant human HTR1A. HEK293-CNG cells express a modified CNG (Cyclic Nucleotide Gated) channel that opens in response to elevated intracellular cAMP levels and consequently result in ion flux and cell membrane depolarization which can be easily measured with fluorescent Membrane Potential Dye (Cat# MBS430187). The assay allows both end-point and kinetic measurement of intracellular cAMP changes with a FLIPR, or a fluorescence microplate reader