You may have spotted a couple of these little creatures whilst undertaking yesterday’s quiz.
These drugs lend themselves very well to a discussion of structure activity relationships, as there a large number of ways the basic catecholamine structure has been altered, to produce a range of drugs with different pharmacokinetic and pharmacodynamic properties
BT_PO 1.53 describe the pharmacology of adrenergic agonists
Here is one true statement to get you oriented:
Phenylethylamine can be considered the parent drug on which all sympathomimetics are based.
Here is the molecule with the carbons numbered
Maximal ⍺ and B potency is conferred by OH substitutions on the 3′ and 4′ positions of the benzene ring T/F
Sympathomimetics can be chiral around either the ⍺ or B carbon T/F
A very large substitution on the terminal amine promotes B1 selectivity T/F
A methyl substitution at the ⍺ carbon prevents metabolism by monoamine oxidase and prolongs duration of action T/F
Absence of hydroxyl groups on the benzene ring improves oral bioavailability by preventing metabolism by COMT T/F