PHRD6925 MedChem Lecture 3 - Drugs affecting adrenergic neurotransmission

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  1. identify:
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  2. phenylethanolamine agonists minimally require this for agonist activity
    primary or secondary aliphatic amine separated by 2 C's from the substituted benzene ring
  3. what configuration does the hydroxyl group need to be in for maximum activity?
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    R configuration
  4. substitution at which R group can prevent MAO?
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    R2 (and partially R1)
  5. which R group affects selectivity?
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  6. what types of drugs are these?
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    • Image Upload1 adrenergic agonists
    • (phenylephrine, metaraminol, methoxamine)
  7. Image Upload1-agonists are used in what treatment?
    • hypotension during surgery, shock
    • strong vasoconstrictors
  8. purpose of amine in fused ring system in these Image Upload2- agonists
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    prevents MAO activity
  9. purpose of methyldopa
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    • prodrug that can cross BBB and be metabolized into norepinephrine
    • anti-hypertensive Image Upload2-agonist
  10. what are most Image Upload2-adrenergic agonists used for?Image Upload
    bronchodilators (asthma, constrictive pulmonary disorders)
  11. portion of Image Upload2-agonists that make them more Image Upload selective
    Image Upload
    heavily substituted N
  12. portion that prevents COMT activity in Image Upload2 agonists
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  13. purpose of large, bulky group in salmeterol
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    • slows MAO for a longer duration of action 
    • (long acting Image Upload2 agonist)
  14. identify:
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    • mixed-acting sympathomimetics (both Image Upload and Image Upload activity)
    • amphetamine and methamphetamine
  15. identify:
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    • Image Upload1-antagonists - antihypertensives
    • (prazosin, terazosin, doxazosin)
  16. identify:
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    Image Upload-adrenergic antagonists
  17. if you see a quinazoline group, what kind of receptor blocker is it?
    Image Upload
    Image Upload1-antagonist
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PHRD6925 MedChem Lecture 3 - Drugs affecting adrenergic neurotransmission
2015-03-05 05:48:13

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