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5 Cards in this Set

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Acetylcholinesterase as a target - Reversible inhibitors
- Irreversible inhibitors
Reversible inhibitors are used therapeutically....

Organophosphates are irreversible inhibitors used as nerve gases and insecticides
Synthesis of Acetylcholine
-Rate limiting factor
-Inhibitor of reuptake
-Vesicular transport
-Inhibitor of vesicular transport
-Choline AcetylTransferase acetylates choline with acetylCoA

-exogenous supply of choline

-High affinity choline transporter reuptakes choline from degraded synaptic Ach

-Hemicholinium inhibits HACT leading to depletion of ACh stores

-VAChT transports ACh into vesicles and is inhibited by Vesamicol
Botulinium toxin
-Activated intracellulary, cleaves SNARE proteins and prevents Ach release
Nicotinic Receptors (AChR)
1. Structure
2. Subtype distribution on muscle
3. Subtype distribution on neurons
1. Pentameric ligand gated cation channels that mediate fast muscle contraction

2.Skeletal muscle expresses alpha, beta, delta and either epsilon (postnatal) or gamma (embryonic

3.Neurons express combinations of other alpha and beta subtypes but not delta or gamma
Muscarinic Receptors
-Two groups and their Secondary effectors
G-protein coupled receptors

-M1/3/5 stimulate phospholipases C/D and Arachodonic Acid

-M2/4: dual inhibition
---Gi-alpha inhibits adenyl cyclase

---Go-beta-gamma open K+ channels to inhibit electrical excitation