PHRD6925 MedChem Lecture 3 - Drugs affecting adrenergic neurotransmission
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phenylethanolamine agonists minimally require this for agonist activity
primary or secondary aliphatic amine separated by 2 C's from the substituted benzene ring
what configuration does the hydroxyl group need to be in for maximum activity?
substitution at which R group can prevent MAO?
R2 (and partially R1)
which R group affects selectivity?
what types of drugs are these?
- 1 adrenergic agonists
- (phenylephrine, metaraminol, methoxamine)
1-agonists are used in what treatment?
- hypotension during surgery, shock
- strong vasoconstrictors
purpose of amine in fused ring system in these 2
prevents MAO activity
purpose of methyldopa
- prodrug that can cross BBB and be metabolized into norepinephrine
- anti-hypertensive 2-agonist
what are most
2-adrenergic agonists used for?
bronchodilators (asthma, constrictive pulmonary disorders)
2-agonists that make them more
heavily substituted N
portion that prevents COMT activity in
purpose of large, bulky group in salmeterol
- slows MAO for a longer duration of action
- (long acting 2 agonist)
- 1-antagonists - antihypertensives
- (prazosin, terazosin, doxazosin)
if you see a quinazoline group, what kind of receptor blocker is it?
What would you like to do?
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