Ops

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Ops

  1. 1. OpioidreceptorsClassificationCellularmechanismsAgonists and antagonists<br />Flavio Guzmán, MD<br />
  2. 2. Presentationoutline<br />General classification<br />Cellular actions of opioid receptors<br />Mu receptors<br />Delta receptors<br />Kappa receptors<br />Review <br />ORL-1 receptors<br />
  3. 3. Classification: opioidreceptors<br />
  4. 4. Opioidreceptors are 7 transmembranereceptors<br />3<br />2<br />1<br />N- terminus<br />4<br />3<br />1<br />2<br />5<br />6<br />7<br />3<br />1<br />2<br />C- terminus<br />
  5. 5. Before opioid receptor activation<br />Presynaptic neuron<br />
  6. 6. After opiod receptor activation<br />Morphine<br />
  7. 7. Glutamate, Ach, NE, 5-HT, substance P<br />
  8. 8. Mu opioid agonists<br />Exogenous drug<br />Endogenous peptide<br />
  9. 9. Mu antagonist<br />
  10. 10.
  11. 11.
  12. 12. Delta receptors<br />Exogenous drug<br />Endogenous peptide<br />
  13. 13. Delta antagonist<br />
  14. 14.
  15. 15.
  16. 16. Kappa receptor agonists<br />Exogenous drug<br />Endogenous peptides<br />
  17. 17. Kappa antagonist<br />
  18. 18.
  19. 19.
  20. 20. Receptor review<br />Endogenous peptides<br />Antagonists<br />Exogenous drug agonists<br />
  21. 21. ORL1 receptor<br />Opioid-like-subtype-1 receptor<br />Also known as: <br />nociceptin receptor (NOP)<br />Orphanin FQ receptor<br />
  22. 22. ORL1 receptor- Natural ligand<br />Nociceptin or orphanin FQ only acts at the ORL1 receptor.<br />
  23. 23. ORL1 receptor<br />Effects upon activation:<br />Central modulation of pain.<br />Effects on locomotion, stress, anxiety, feeding, learning and memory, reward/addiction and urogenital activity.<br />
  24. 24. References and further reading<br />Katzung, B. Basic and Clinical Pharmacology. 11th ed. McGraw Hill Medical, 2009<br />Koneru A, Sreemantula S, Rizwan. Endogenous Opioids: Their Physiological Role and Receptors. Global J. Pharmacol., 3 (3): 149-153, 2009<br />McDonald J, Lambert DJ. Opioid Receptors. Continuing Education in Anaesthesia, Critical Care & Pain 2005 5:1<br />Trescot A, Sukdeb D. Opioid Pharmacology. Pain Physician 2008; 11:S133-S153<br />

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