Med. Chem. II Week Three
Review and Study Guide

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B. Drugs Affecting Adrenergic Receptor (AR) Functions (continued)

1. Beta-adrenoceptor Agonists

a. ß₁-AR Agonists

1) SAR (branched alkyl substituent on N, ß-OH)

2) Dobutamine

b. ß₂-AR Agonists

1) SAR

- ß-Arylethanolamine pattern

- branched alkyl secondary amine

- structural variation of catechol to enhance chemical and metabolic stability (pg. 38)

2. Alpha-AR Antagonists

a. Ergot alkaloids

b. Quinazolines (SAR, biodisposition, basicity, receptor selectivity)

c. ß-Arylethylamines

3. Beta-AR Antagonists

a. Structural derivation from NE

b. SAR

c. Physicochemical properties (optical isomerism, basicity, relative solubility)

d. Dual alpha/beta-AR antagonists (pharmacological role of optical isomerism)

e. Biotransformation pathways for ß-blockers

C. Drugs Affecting Neuronal Signal Transduction Processes

1. Sites of Drug Action

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