MED. CHEM. I STUDY GUIDE FIVE

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DRUGS AFFECTING THE PERIPHERAL NERVOUS SYSTEM

A. DRUGS AFFECTING CHOLINERGIC NEUROTRANSMISSION

1. Neurotransmission by Acetylcholine

a. Biosynthesis from choline + AcCoA (choline acetyltransferase)
b. Storage in presynaptic vesicles
c. Release (involvement of Ca++
d. Cholinergic receptors
1) Types and subtypes (nomenclature)
2) Differences in anatomical distribution
3) Signal transduction
a) MAChR - IP3/DAG second messengers
b) NAChR - ion channel structure and function
e. Termination - AChE hydrolysis of ACh, reuptake of choline

2. Cholinomimetic Agents

a. Therapeutic applications
b. Mechanisms of Cholinomimesis
1) Direct-Acting Cholinomimetics (AChR Agonists)
a) SAR of ACh
b) Structural modifications that improve chemical and metabolic stability
c) Structural modifications that influence receptor selectivity
2) Indirect-Acting Cholinomimetics (AChE Inhibitors)
a) AChE hydrolysis of ACh
b) Reversible inhibition of AChE
(1) Structural requirements - aryl carbamate derivatives
(2) Reaction with and inhibition of AChE
(3) Tacrine
c) Irreversible inhibition of AChE
(1) Structural requirements - organophosphate derivatives
(2) Reaction with and inhibition of AChE
(3) 2-PAM-assisted regeneration

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