BT_PO 1.52 and 1.53 Adrenergic agonists

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

Phenylethylamine_numbered.svg

 

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

Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out / Change )

Twitter picture

You are commenting using your Twitter account. Log Out / Change )

Facebook photo

You are commenting using your Facebook account. Log Out / Change )

Google+ photo

You are commenting using your Google+ account. Log Out / Change )

Connecting to %s