MED. CHEM. I STUDY GUIDE FOUR

C. DRUGS AFFECTING BIOGENIC AMINE NEUROTRANSMISSION

1. Neurotransmission by Dopamine

a. Biosynthesis from L-tyrosine

b. Storage in presynaptic vesicles

c. Release (regulation by autoreceptors and presynaptic 5HT₂ receptors)

d. Dopaminergic receptors (subtypes, signal transduction)

e. Termination (reuptake, intra- and extraneuronal catabolism)

2. Antiparkinson Drugs

a. Neurologic defect associated with Parkinson's Disease and rationale for antiparkinson drug therapy

b. L-Dopa and carbidopa

c. Dopamine receptor agonists (ergot alkaloid derivatives)

d. Stimulation of dopamine release (amantadine)

e. Inhibition of dopamine catabolism (MAO inhibitors)

3. Antipsychotic Agents

a. Neurochemical defect of psychotic disorders and rationale for antipsychotic drug action (conventional vs. atypical neuroleptic neurochemical effects)

b. Neurotransmission by Serotonin (details of life cycle)

c. Structural classes of antipsychotic agents

1) Phenothiazine derivatives

a) General structural features

b) Physicochemical properties (relative solubility, basicity)

c) Structure-activity relationships - structural subclasses

d) General aspects of phenothiazine metabolism

e) Phenothiazine products and prodrugs

2) Butyrophenone derivatives (general structure, SAR, properties, metabolism

3) Dibenzazepines derivatives

4) Benzamide derivatives

5) Serotonin-Dopamine Antagonists (SDAs) - clozapine, risperidone, olanzapine.

4. Antidepressants

a. Mechanism of action of antidepressants

b. Biogenic Amine Reuptake Inhibitors

1) First-generation agents (general structural features, subclasses, neurochemical actions)

2) Second-generation agents (non-tricyclics, SSRIs, etc.)

3) General physicochemical properties

4) Structure vs. neurochemical effects

c. Monoamine Oxidase Inhibitors

a) First-generation agents

b) Second-generation MAOIs (enzyme selectivity, mechanism of enzyme inhibition).

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