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Advances in the structural understanding of opioid allostery

4DQSAR

Bluelighter
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Feb 3, 2025
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Again very recent research. But PAMs such as BMS-986122 are items of commerce. But do bear in mind this is still just in vitro and as they conclude, we also have compounds that slow down the metabolism of endorphins. The French even have an OTC medication that does just this. It doesn't cross the BBB but since metabolism of endomorphins occur outside the BBB, it's entirely possible that at a sufficient dose, it might allow the consumer to 'get high of their own supply'. They also developed a version that DOES cross the BBB but the research seemed to just peter out. Why, I don't know.

But as with the other paper, it's possible that compounds that are, when consumed alone, totally without psychoactive effect MAY be able to make antagonists behave much more like agonists. Now who knows where this will lead. Well, statistically, likely nowhere - but if it increases our understanding of the MOR receptor, it has value.
 
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