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The mu opioid receptor (MOR), encoded by the OPRM1 gene, is a G protein-coupled receptor and the primary target for opioid analgesics and endogenous opioid peptides. It mediates analgesia, reward, respiratory depression, sedation, and gastrointestinal effects. Genetic variations in OPRM1 influence individual opioid sensitivity and addiction risk. MORs form dimers with other GPCRs, modulating their pharmacology. Biased agonism is being explored to separate analgesic effects from adverse side effects.
Agonist binding to the mu opioid receptor leads to Gi/o protein activation, inhibition of adenylyl cyclase, decreased cAMP production, and neuronal hyperpolarization via potassium channel activation and/or calcium channel inactivation.
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