Acetylcholinesterase Inhibitors (Lecture 7)
Acetylcholine (ACh) Mechanism of Action
1. **How ACh Acts as a Neurotransmitter:** - **Synthesis:** ACh is synthesized from acetate and coenzyme A (CoA) in the presence of water. - **Storage:** ACh is stored in vesicles within the presynaptic neuron....
Acetylcholinesterase Inhibitors (Lecture 7)
Acetylcholine (ACh) Mechanism of Action
1. **How ACh Acts as a Neurotransmitter:**
- **Synthesis:** ACh is synthesized from acetate and coenzyme A (CoA) in the presence of water.
- **Storage:** ACh is stored in vesicles within the presynaptic neuron.
- **Release:** ACh is released into the synaptic cleft upon presynaptic neuron stimulation.
- **Receptor Activation:** ACh binds to either nicotinic or muscarinic receptors on the postsynaptic
cell, depending on the cell type.
- **Metabolic Inactivation:** ACh is quickly inactivated by acetylcholinesterase (AChE) into inactive
substances (acetate and choline).
2. **Identifying Postsynaptic Receptors:**
- The type of cholinergic receptor (nicotinic or muscarinic) depends on the target cell. Nicotinic
receptors are typically present in skeletal muscle and autonomic ganglia, whereas muscarinic receptors
are found in smooth muscle, cardiac muscle, and glandular tissues.
3. **ACh Synthesis and Breakdown:**
- **Synthesis Reaction:** Acetate + CoA + H₂O → ACh
- **Breakdown Reaction:** ACh + AChE → Acetate + Choline
- Both acetate and choline are metabolic breakdown products and are not active neurotransmitters.
### Acetylcholinesterase Inhibitors (AChEIs)
1. **General Concepts:**
- ACh is the active neurotransmitter.
- AChE metabolizes ACh, terminating its action.
- Inhibiting AChE results in increased levels of ACh in the synapse, leading to prolonged activation of
nicotinic and muscarinic receptors.
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