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Effects of activation of opiate receptors and drugs acting on them Aron Takacs Opioid Receptors • G protein-coupled receptors • Activated by opioid peptides • Mainly found in: Brain Spinal cord Digestive Tract • Main types: Delta opioid receptor Kappa opioid receptor Mu opioid receptor Nociceptin opioid receptor Mu receptor bound to antagonist Opiates • Types: Agonist Antagonist • Endogenous opioids: Dynorphins Enkephalins Endorphins Nociceptin nociceptin Effects of activation of opiate receptors • Analgesia = Pain killer • Sedation • Reduces the excitability of neurons • Can create strong physical addiction • GABA inhibition mechanism: Suppresses the release of GABA GABA regulates the release of dopamine Increases dopamine levels morphine Drugs • Morphine: • Binds to Mu and Delta receptors Analgesia Sedation Standard against all other opiates Heroin: 2-4x more potent then morphine Used in the past as cough medication antidiarrheal cocaine addiction medication heroin