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DAMGO

Synthetic opioid peptide

Synthetic opioid peptide

DAMGO ([D-Ala2, N-MePhe4, Gly-ol]-enkephalin) is a synthetic opioid peptide with high μ-opioid receptor specificity. It was synthesized as a biologically stable analog of δ-opioid receptor-preferring endogenous opioids, leu- and met-enkephalin. Structures of DAMGO bound to the μ opioid receptor reveal a very similar binding pose to morphinans.

Its structure is H-Tyr-D-Ala-Gly-N-MePhe-Gly-ol.

DAMGO has been used in experimental settings for the possibility of alleviating or reducing opiate tolerance for patients under the treatment of an opioid. Such treatment on rats, adding DAMGO to morphine administration, showed that after seven days morphine had as much of an effect at the same dosage as the first day when administered together with DAMGO to the rats, whereas a separate control group of rats that were administered the same dosage of morphine over the course of the same week, but without DAMGO, displayed an increased tolerance and lessened analgesic efficacy toward the end of that week.

References

References

  1. (April 1981). "Analogues of β-LPH61–64 possessing selective agonist activity at μ-opiate receptors". European Journal of Pharmacology.
  2. (June 2018). "Structure of the μ-opioid receptor–Gi". Nature.
  3. (2022-11-10). "Molecular recognition of morphine and fentanyl by the human μ-opioid receptor". Cell.
  4. Radler, Don. (25 January 2002). "Reducing Tolerance To Morphine Could Aid Pain Therapy". UniScience News Net, Inc..
  5. (December 2001). "Endocytosis of the Mu Opioid Receptor Reduces Tolerance and a Cellular Hallmark of Opiate Withdrawal". Neuron.
  6. (January 2002). "Regulation of Opioid Receptor Trafficking and Morphine Tolerance by Receptor Oligomerization". Cell.
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synthetic-opioids opioid-peptides mu-opioid-receptor-agonists
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