PHRD6925 MedChem Lecture 3 - Drugs affecting adrenergic neurotransmission

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daynuhmay
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297613
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PHRD6925 MedChem Lecture 3 - Drugs affecting adrenergic neurotransmission
Updated:
2015-03-05 00:48:13
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medchem
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medchem
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  1. identify:
    catecholamine
  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?
    R configuration
  4. substitution at which R group can prevent MAO?
    R2 (and partially R1)
  5. which R group affects selectivity?
    R1
  6. what types of drugs are these?
    • 1 adrenergic agonists
    • (phenylephrine, metaraminol, methoxamine)
  7. 1-agonists are used in what treatment?
    • hypotension during surgery, shock
    • strong vasoconstrictors
  8. purpose of amine in fused ring system in these 2- agonists
    prevents MAO activity
  9. purpose of methyldopa
    • prodrug that can cross BBB and be metabolized into norepinephrine
    • anti-hypertensive 2-agonist
  10. what are most 2-adrenergic agonists used for?
    bronchodilators (asthma, constrictive pulmonary disorders)
  11. portion of 2-agonists that make them more  selective
    heavily substituted N
  12. portion that prevents COMT activity in 2 agonists
    methyl-OH
  13. purpose of large, bulky group in salmeterol
    • slows MAO for a longer duration of action 
    • (long acting 2 agonist)
  14. identify:
    • mixed-acting sympathomimetics (both  and  activity)
    • amphetamine and methamphetamine
  15. identify:
    • 1-antagonists - antihypertensives
    • (prazosin, terazosin, doxazosin)
  16. identify:
    -adrenergic antagonists
  17. if you see a quinazoline group, what kind of receptor blocker is it?
    1-antagonist

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