Opioid introduction and receptors 3

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kyleannkelsey
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269275
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Opioid introduction and receptors 3
Updated:
2014-04-04 22:41:46
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Opioid introduction receptors
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Opioid introduction and receptors
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Opioid introduction and receptors
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  1. ________ substituents with a _________ electron density can bind to the “antagonist site”
    • Nitrogen
    • High
  2. What residue creates the hydrogen acceptor site for phenolic opioid agonists and antagonists?
    HIS
  3. What residue creates the hydrogen donor site for the carbonyl oxygen in fentanyl-like opioids?
    HIS
  4. The same Histadine residue is responsible for creating the Hydrogen receptor and Hydrogen Donor sites.
    True
  5. The Histadine responsible for the Hydrogen Donor and Acceptor sites is flanked by what type of residues?
    Large number of aliphatic (lipophilic) residues
  6. Does the kappa receptor have a Histadine that is comparable in activity to the mu receptor?
    Yes
  7. Two Van der Waals sites are available for binding the aromatic benzene ring of opioids at mu receptors, what residues are responsible for this ineraction?
    2 TRPs
  8. Enkephalin peptides have two aromatic residues that create a Van Der Waals site on the Delta receptors, what are those residues?
    TYR and PHE
  9. What residue on the enkephalin binds to the Van Der Waals 1 (TRP) site?
    TYR
  10. What residue on the enkephalin binds to the Van Der Waals 2 (TRP) site?
    PHE
  11. The phenyl ring found in rigid opioids is held in what orientation?
    Axial to the nitrogen-containing ring
  12. The phenyl ring of rigid opioids binds what site on the mu receptor?
    Van der Waals site1 (TRP)
  13. All multicyclic opioids (e.g., morphine and codeine derivatives) are classified as flexible or rigid?
    Rigid
  14. Since TYR of enkephalins has a phenolic OH, all of the multicyclic opioids will also require a ________ for high affinity binding to this Van der Waals site.
    Phenolic OH
  15. Flexible opioids (e.g., meperidine, fentanyl, and methadone) have a phenyl ring that can become _________ to the nitrogen-containing ring.
    Equatorial
  16. The phenyl ring of flexible opioids is stable (lower energy) in what position?
    Equitorial
  17. The equatorial phenyl ring of Flexible opioids binds what site on the mu receptor?
    Van der Waals site2 (TRP)
  18. The equatorial phenyl ring of Flexible opioids binds to the Van Der Waals 2 site (TRP), where PHE of an enkephalin would normally bind, does it need to have an OH group?
    NO, because PHE does not have a phenolic OH
  19. What residue on the mu receptor hydrogen bonds with the C6-OH or keto of some pentacyclic opioid agonists?
    ASN
  20. What residue on the Kappa receptor hydrogen bonds with the C6-OH or keto of some pentacyclic opioid agonists?
    LEU
  21. ASN that H-bonds with C6-OH of some pentacyclic opioid agonists also interacts hydrophobically with the phenyl ring of opioids in what class?
    Anilinopiperidine class (the fentanyls)
  22. Fentanyls bind to another TYR residue through what type of bonds?
    H-bonds
  23. What position must a phenyl ring be in on a fentanyl opioid to bind with the Van Der Waals 2 site?
    Equatorial with respect to the nitrogen-containing ring
  24. The phenyl ring of fentanyl binds to the Van der Waals site ______.
    2
  25. What residue hydrogen bonds with the C14-OH found on highly potent mu agonists and antagonists?
    TYR
  26. What residue hydrogen bonds with the C14-OH found on Kappa agonists and antagonists?
    GLU
  27. (True/False) LYS233 is highly conserved among opioid receptors.
    True
  28. The carbons of this LYS are believed to interact with what part of the opioid?
    C-ring of multicyclic opioids
  29. Hydrophobic residues, including ILE322, line the mu receptor active site cavity, and are known to interact with the carbons on the _____________ of our opioids.
    Nitrogen-containing ring
  30. The various ILE and VAL residues add to the ___________ of the receptor binding pocket.
    Lipophilicity

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