MED. CHEM. I STUDY GUIDE
Quiz Three

C. DRUGS AFFECTING AMINO ACID NEUROTRANSMISSION

1. Amino Acid Neurotransmitters

a. Excitatory (L-Glu, L-Asp)

b. Inhibitory (GABA, Gly)

c. Structural characteristics

2. GABA Neurotransmission

a. Biosynthesis

b. Storage

c. Release

d. Receptors (types, signal transduction)

e. Termination, metabolism

3. Anxiolytics, Sedatives/Hypnotics

a. Alcohols

1) Structural features that increase lipid solubility of alcohols

2) Structural features that increase chemical stability of alcohols

b. Barbiturates

1) General structure and nomenclature

2) Important physicochemical properties

a) Acidity - ionization, salt formation

b) Lipid solubility - roles of C2 and C5-substituents

3) Structure vs. activity (role of C5-substituents)

4) Termination of CNS activity (metabolism, tissue redistribution)

5) Mechanism of barbiturate action (facilitation of GABA neurotransmission)

c. Benzodiazepines

1) General structural aspects, nomenclature

2) Important physicochemical properties

a) Relative solubility

b) Acid-base character and formation of dosage forms

3) Clinically-relevant reactions (ring hydrolysis, prodrug conversion)

4) Structure vs. CNS activity

a) Essential structural features

b) Structural features that influence biodisposition

c) Metabolism, structure and duration of action

d) Benzodiazepine antagonists

e) Conformational aspects

5) Mechanism of benzodiazepine action (facilitation of GABA neurotransmission)

4. Anticonvulsants

a. Mechanism of action in epilepsy

b. Structural classes

1) Ureides

a) Barbiturates

b) Hydantoins

c) Oxazolidinediones

d) Succinimides

e) Acylureides

2) Benzodiazepines

3) Miscellaneous

a) Carbamazepine

b) GABA analogues

c) Newer agents (lamotrigine, felbamate)

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