MED. CHEM. I STUDY GUIDE FIVE
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DRUGS AFFECTING THE PERIPHERAL NERVOUS SYSTEM
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- 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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