Morphine metabolites

@article{Christrup1997MorphineM,
  title={Morphine metabolites},
  author={Lona Louring Christrup},
  journal={Acta Anaesthesiologica Scandinavica},
  year={1997},
  volume={41}
}
  • L. Christrup
  • Published 1 January 1997
  • Biology, Chemistry
  • Acta Anaesthesiologica Scandinavica
Morphine is a potent opioid analgesic widely used for the treatment of acute pain and for long‐term treatment of severe pain. Morphine is a member of the morphinan‐framed alkaloids, which are present in the poppy plant. The drug is soluble in water, but its solubility in lipids is poor. 
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TLDR
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ANALGESIC ACTIVITY OF MORPHINE-6-GLUCURONIDE
Morphine-6-glucuronide is more mu-selective and potent in analgesic tests than morphine.
TLDR
6-glucuronidation of morphine confers to this widely used analgesic increased potencies both in terms of receptor binding (selectivity) and of antinociceptive properties, and Na+ ions and Gpp(NH)p inhibit similarly the binding of morphine and M6G at the mu sites, suggesting that M 6G is a mu agonist.
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TLDR
Results imply that morphine-6 beta-glucuronide elicited its analgesic actions through the same receptor mechanisms as morphine, which strongly suggests that this metabolite plays an important role in morphine's actions.
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TLDR
The radiolabelled opioid receptor binding affinities of morphine and its active metabolite morphine 6-glucuronide at the total mu, mu 1, mu 2 and delta receptors were determined and provided a possible explanation for the reduced respiratory depression and vomiting seen following morphine6-glUCuronide in man.
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