Drugs that activate receptors in the brain are termed agonists. Agonist bind to receptors and turn them on-they produce an effect. Full mu opioid agonists acitvate mu receptors. Opioids with the greatest abuse potential are full agonists-morphine, heroin, oxycodone, hydromorphone, methadone. On the other end of the spectrum are antagonist. An antagonist also binds to receptors but instead of activating receptors, they effectively block them-naltrexone and naloxone are antagonists. They are like a key that fits the lock but doesnt open the lock and prevents any other keys from being inserted into the lock at the same time. Does that help?
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