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I am pretty unfamiliar to pharmacology. I'm doing a research on drug abuse, particularly opioids' mechanism of action. I encountered several times evidences that come from studies using antagonists especially naloxone that are to prove something is 'a specific opioid effect':

Opioid-induced miosis in the human ... This action is a specific opioid effect as demonstrated by its antagonism by naloxone.

I wanted to know the rationale behind these kind of conclusions. Also an elaboration on the role antagonists play in drug research will be appreciated.

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An antagonist is a substance that blocks a particular pathway (a receptor). You can therefore test whether a particular drug acts through the opioid system by using an opioid antagonist. If your substance still works despite the presence of the antagonist (which should block the opoiod receptors), you can conclude that it is not working thorough the opioid system.

Conversely, if your drug is blocked by an opioid antagonist, that is good evidence that your drug works through the opioid system.

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What many drugs and compounds do is bind to cell receptors. These receptors then change shape and various things may happen in the cell as a result (including relaying a message to other cells).

Something that binds to a receptor and causes activity is called an agonist. Something that binds to a receptor and causes a partial response is called a partial agonist. Something that binds to a receptor but does not cause activity is called an antagonist as it takes up those receptor sites meaning that nothing else can bind to them and cause and effect.

An opioid effect is one of many effects caused by opioids. Naloxone is an opioid antagonist. It binds to the same receptors as opiates but without causing an effect. If a normal person has naloxone it won't actually cause an effect. If someone who has taken an opiate takes naloxone however, the naloxone will compete for receptor spots, knocking off the opiate and reversing the opiate effect. Also, if someone takes naloxone and then immediately has an opiate, that opiate will not work particularly well as some of those receptors are already taken up with naloxone.

Hope that helps.

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  • $\begingroup$ Very precise and simple explanation. Thank you so much. $\endgroup$
    – Ehsan88
    Aug 31, 2013 at 17:32
  • $\begingroup$ @EhsanAbd No worries! $\endgroup$
    – Tomcat
    Aug 31, 2013 at 19:48

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