In-direct Acting Adrenergic Receptor Agonists

Question 1

Amphetamine

Answer 1

Promote release of NE via reverse action of plasma membrane transporter

Clinical uses:
 Amphetamines: ADHD, narcolepsy, anorexiant
 Others: Nasal decongestants

Question 2

D-(-)-Ephedrine

Answer 2

 Alkaloid obtained from the stems of Ephedra. Also found in mahuang.
 D-(-)-Ephedrine has desired (R)-configuration at b-OH and (S)-configuration at the a carbon for direct agonist
 activity at adrenergic receptors
 L-(+)-Pseudoephedrine is the
 (S,S)-diastereoisomer; (S)- configuration of b-OH reduces agonist activity-major mechanism is via reversal of the transporter

Question 3

L-(+)-Pseudoephedrine

Answer 3

 Alkaloid obtained from the stems of Ephedra. Also found in mahuang.
 D-(-)-Ephedrine has desired (R)-configuration at b-OH and (S)-configuration at the a carbon for direct agonist
 activity at adrenergic receptors
 L-(+)-Pseudoephedrine is the
 (S,S)-diastereoisomer; (S)- configuration of b-OH reduces agonist activity-major mechanism is via reversal of the transporter