Mu-Type Opioid Receptor (OPRM1) Antibody

Background

OPRM1, or the mu-opioid receptor, is the primary target for endogenous opioid peptides like endorphins and exogenous opioids such as morphine, fentanyl, and heroin. OPRM1 is highly expressed in pain-processing regions of the CNS, including the brainstem, thalamus, and spinal cord, where it mediates analgesia, euphoria, and sedation. OPRM1 couples to Gi/o proteins, inhibiting adenylate cyclase, reducing cAMP levels, and modulating ion channels to decrease neuronal excitability and neurotransmitter release. Activation of OPRM1 produces potent analgesic effects but also carries risks of tolerance, dependence, and respiratory depression. Dysregulation of OPRM1 signaling is central to opioid addiction, chronic pain, and reward pathways. Selective modulation of OPRM1 has therapeutic potential for improving pain management while reducing side effects such as tolerance and dependence. Biased agonists that preferentially activate analgesic pathways over adverse effects are under development to enhance safety. OPRM1 remains a key target for opioids and therapies addressing addiction and pain disorders.