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Adrenergic Neurotransmission
Catecholamines and Adrenergic Receptors (subtypes and distribution)
23
Pharmacology
Graduate
10/29/2011

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Cards

Term
What is the MOA of adrenergic neurotransmission?
Definition
Tyrosine enters and is reduced by Tyrosine hydroxylase to Dopa; Dopa is converted to Dopamine which is then converted to NE and stored in vessicles until released into the synapse.
Term
What is the MOA for terminating the effect of NE?
Definition
Combination of reuptake and enyzmatic degredation.
*NET (NE transporter) reuptake
*MAO (monoamine oxyidase) degredation
Term
List 6 catecholamines.
Definition
1. catechol
2. phenylethylamine
3. norepinephrine
4. epinephrine
5. isoproterenol
6. dopamine
Term
A cocaine of a tricyclic antidepressant would be classified as an ___. Why?
Definition
*indirect working agonist
*because it will bind to the NE reuptake transporter thus increase the amount of NE remaining available in the synapse
Term
Epinephrine is a hormone from the ___.
Definition
Adrenal medula.
It lacks a methyl group that NE has.
Term
Alpha and Beta receptors are all ___ receptors.
Definition
G-protein coupled
Term
What is the typical location of the Alpha 1 receptor? What are the subtypes?
Definition
*post-synaptic effector cells of most vascular smooth muscle; puliary dilator muscle; protate
* 1A, 1B, 1D
Term
What is the result of ligand binding/action of the Alpha 1 receptor?
Definition
*increase in intracellular Ca2+, vasoconstriction; contraction
Term
What is the typical location of the Alpha 2 receptor? What are the subtypes?
Definition
*post-synaptic receptors in CNS, adrenergic nerve terminals
* 2A, 2B, 2C
Term
What is the result of ligand binding/action of the Alpha 2 receptor?
Definition
*inhibition of adenylate cyclase; *decrease in cAMP/opens K+ channel/inhibition of neurotransmitter release
*stimulation produces autoregulatory effect in terms of regulating the activity of simpathetic outflow
*inhibits stimulation of simpathetic outflow
*inhibit by hyperpolarizing
Term
What is the typical location of the Beta 1 receptor?
Definition
*heart, juxtablomerular cells, lipocytes, CNS, ciliary body
Term
What is the result of ligand binding/action of the Beta 1 receptor?
Definition
*stimulation of the adenylate cyclase; increase in cAMP/Positive chronotropy and inotropy; renin release
*increase heart rate and force of contraction thus combined leads to increaesed cardiac output.
Term
What does cardiac output depend on?
Definition
stroke volume and heart rate
Term
What is the typical location of Beta 2 receptors?
Definition
*respiratory uterine and vascular smooth muscle
*mainly present in areteries going to skeletal muscle as opposed to vascular smooth muscle in the Alpha 1
Term
What is the result of ligand binding/action of the Beta 2 receptor?
Definition
*vaso dilation of the arteries going to skeletal muscle
*stimulation of adenylate cyclase; increase in cAMP/smooth muscle relaxation
Term
What is the typical location of the D1(dopamine 1) receptor?
Definition
*renal, mesenteric, coronary and cerebral blood vessels
Term
What is the result of ligand binding/action of the D1 receptor?
Definition
*vasodilation of renal arteries with increase in blood flow and filtration rate (promotes excretion of fluids)
*inhibition of NA/H pump
Term
What is the typical location of D2 (dopamine 2) receptor?
Definition
CNS
Term
What is the result of ligand binding/action of the D2 receptor?
Definition
*inhibition of adenylate cyclase; decreasein cAMP; modulates neurotransmitter release
Term
How do A2 and B signaling oppose each other?
Definition
*A2 inhibits adenylate cyclase and B1 stimulates it
Term
What are the classes of adrenergic agaonists?
Definition
1. direct acting
2. mixed acting
3. indirect-acting
Term
What are the classes of indirect-acting Adrenergic Agonists?
Definition
1. releaseing agents
2. utake inhibitor
3. MAO/COMT inhibitors
Term
What are the classes of Direct Acting Adrenergic Agonists?
Definition
1. Secective
2. Non-selective
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