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21 Cards in this Set
- Front
- Back
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Manipulation of Autonomic Synapse |
-Presynaptic neuron (synthesis/storage/release) -Postsynapthic (signal detection/action of cell activity) |
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Neurtransmission Pharmacologic Targets |
-Block synthesis/storage: rate limiting (long term effects -Block release: (rapid and effective action) -Block reuptake: Increase synaptic transmitter conc. (selective/nonselective) -Metabolism interfere: Reversible/irreversible (increases transmitter conc.) -Interfere with action: Receptor Ant/agonists (highly specific) |
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Define: Agonist/Antagonist |
Agonist: Activates receptor Antagonist: blocks receptor |
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Mode of Action of Ant/agonists NOT THE SAME AS Ant/agonism |
Direct acting: physically binds to target Indirect acting: interacts with non target site |
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Indirect Agonist |
Physostigmine -ACH receptor effector -Mediated through inhibition of cholinesterase -Increases local ACH -therefore agonist for ACH receptor |
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Acetylcholine |
-Present in neuromuscular junction and CNS -Synthesized in axon terminal -Diffuses across synaptic cleft -Choline + acetyl CoA (choline acetyl transferase) ---> Acetylcholine + CoA |
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Acetylcholine degradation |
Acetylcholinesterase (turnover time of 150 microseconds) (post synaptic) |
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Cholinergic transmission |
1.Precursor transport (rate limiting)[hemocholinium] 2. Synthesis 3. Storage (Vesamicol) 4. Release (botulinum toxin) 5a. receptor action (Antagonists: Atropine/succinylcholine/trimethaphan. Agonist: Carbachol/pilocarpine) 5b. Degradation by AchE. ACHE inhibitors: reversible: neostigmine. Irreversible: Organophosphate |
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Cholinergic receptors: Two for ACH Nicotonic/Muscarinic |
Nicotinic: Ion channels. Ionotropic Muscarinic: G-protein. Metabotropic |
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Nicotinic receptors |
-Found on motor end plates (somatic targets) -All ganglionic neurons for both (para/sympathetic) |
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Major G-protein types |
Gs: Activates adenylyl cyclase, increase cAMP Gi: Inhibitis adenylyl cyclase, decrease cAMP Gq: Activates phospholipase CB, increase IP3 levels and intracellular Ca+ levels |
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Nicotinic Receptors |
Nn: Neuronal (fire) Nm: Skeletal muscle (contract) Both ligand gated ion channels - 2 Ach binding is stimulatory |
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Muscarinic Receptors (Gq) |
M1,3,5 --> activate Gq M3: located on smooth muscle glands (cause contration/secretion) |
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Muscarinic Receptor (Gi) |
M2,4 --> Activate Gi --> inhibit Adenylate cyclase (increase K+ permeability) M2: on heart, decrease activity |
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Adrenergic Transmission Drug intervention |
1. Tyrosine (Metyrosine [inhibitory]) TH rate limiting 2. Dopa --> DA (reserpine [inhibit]) 2. Vesicle DA--> NE (amphet/tyra/ephedrine [Stimulatory]) 3.Release (Bretylium/guanethidine) 4. NE 5a. Receptor action (Antagonist: phentolamine/propranolol. Agonist: isoproterenol/albuterol) 5b. Reuptake (Cocaine/SSRI/TCA's (imipramine) |
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Adrenergic Receptors division: |
a --> a1, a2 b --> b1,b2,3 GPCR |
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Alpha-1 |
Agonist: Contraction/Secretion Works in: smooth mussle/blood vessels/glands |
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Alpha-2 |
Agonist: Release neurotransmitters Mostly presynaptic Increase K+ permeability |
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Beta-1 |
Agonist: Release PKA --> phosphorylate proteins Heart: Increase Heart Rate/Force contraction Kidney: Renin release |
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Beta-2 |
Agonist: Release PKA --> phosphorylate proteins Smooth muscle: Relaxation Liver: Glycogenolysis/gluconeogenesis |
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Beta-3 |
Agonist: Release PKA --> phosphorylate proteins Adipose tissue: Lipolysis |
