Pharmacology of the ANS Flashcards

1
Q

What are the main neurotransmitters of the sympathetic nervous system?

A

NE and Epi

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2
Q

What are the main neurotransmitters of the parasympathetic nervous system?

A

ACh

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3
Q

What type of receptors are found in the sympathetic nervous system?

A

Alpha, Beta, (D)-dopamine, nAChR,mAChR

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4
Q

What type of receptors are found in the sympathetic nervous system?

A

nAChR, mAChR

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5
Q

What ntx is used in ALL PREGANGLIONIC AUTONOMIC FIBERS?

A

ACh

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6
Q

What ntx is used in ALL POSTGANGLIONIC PARASYMPATHETIC FIBERS and only on sweat glands on sympathetic postganglionic fibers?

A

ACh

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7
Q

Where is epinephrine synthesized?

A

Adrenal medulla

Few cells in the brainstem

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8
Q

What is dopamine a precursor for?

A

Epi and NE

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9
Q

On which type of tissues/systems does dopamine act?

A

CNS and vascular smooth muscle

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10
Q

Where are cholinergic neurotransmitters produced? Where are they stored?

A

Cytoplasm

Acetylcholine varicositites

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11
Q

What triggers the release of ACh from presynaptic vesicles?

A

Influx of Ca2+ at the axon terminals

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12
Q

What breaks down ACh?

A

Acetylcholinesterase

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13
Q

Where are nAChR receptors located?

A

CNS

Autonomic Ganglia (Nn)

Adrenal medulla (sympathetic)

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14
Q

What are the functions of nAChRs?

A

Excitatory

Trigger the release of catecholamines

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15
Q

What are nAChr agonists?

A

Acetylcholine

Nicotine

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16
Q

Where are mAChR receptors located?

A

CNS

Autonomic ganglia

Effector organs (cardiac and smooth muscle, gland cells, nerve terminals)

Sweat glands (sympathetic)

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17
Q

What is the function of mAChr?

A

Excitatory and inhibitory in parasympathetics

Sweat secretion in sympathetics

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18
Q

What are some mAChR agonists?

A

Acetylcholine

Muscarine

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19
Q
  • Where are M1 receptors located
  • What are the structural features of M1 receptors
  • What is the mechanism of M1 receptor
A
  • CNS, Ganglia
  • GPCR, Gq
  • Activation of PLC, IP3 and DAG cascade
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20
Q
  • Where are M2 receptors located?
  • What are their structural features?
  • What is the mechanism?
A
  • Heart, nerves, smooth muscle
  • GPCR, Gi/o
  • Inhibit adenylyl cyclase (AC); Decrease cAMP production, activation of K+ channels
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21
Q
  • Where are M3 receptors located?
  • What are their structural features?
  • What is the mechanism?
A
  • Glands, smooth muscle, endothelium
  • GPCR, Gq/11
  • Activation of PLC; IP3 and DAG cascade
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22
Q
  • Where are M4 receptors located?
  • What are their structural features?
  • What is their mechanism?
A
  • CNS
  • GPCR/Gi/o
  • Inhibition of AC; decrease in cAMP production, activation of K+ channels
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23
Q
  • Where are M5 receptors located?
  • What are the structural features of these receptors?
  • What is their mechanism?
A
24
Q
  • Where are Nm receptors located?
  • What are their structural features?
  • What is their mechanism?
A
  • Skeletal muscle, NMJ
  • Ligand gates ion channel
  • Na+, K+ depolarizing ion channel
25
Q
  • Where are Nn receptors located?
  • What are their structural features?
  • What is their mechanism of action?
A
  • Postganglionic cell body dendrites, CNS
  • Ligand gated ion channels
  • Na+,K+ depolarizing channel
26
Q
  • What are the steps of adrenergic neurotransmission?
A
  • Synthesis
  • Storage
  • Release
  • Reuptake
27
Q
  • Where does synthesis of NE and Epi occur? What steps are involved?
A
  • Cytoplasm
  1. Tyrosine transported into cell via Na+ dependent tyrosine transporter
  2. Tyrosine is converted to dopamine
  3. Dopamine transported into vesicles via VMAT 2
  4. Dopamine is converted to NE inside the vescicles (generally speaking, this usually occurs in the adrenal medulla)
28
Q
  • What are the steps in release of NE?
A
  1. Ca2+ influx d/t depolarization at axon terminus
  2. Vesicle fusion with presynaptic membrane
  3. Release of NTX
  4. NTX interacts with alpha or beta adrenergic receptors on postsynaptic cell
29
Q
  • What happens to the remaining NE in the synapse?
    *
A
  • Reuptake via NET (NE Transporter)
  • OR
  • Metabolism via MAO or COMT
30
Q
  • What drug blocks NE reuptake?
A
  • Cocaine
31
Q

What transporter is responsible for the reuptake of dopamine?

A

DAT (Oh shit its dat boi)

32
Q

What drug blocks VMAT 2? What is a consequence of this?

A
  • Reserpine
  • Dopamine cannot be sent to the vesicles to be converted to Epi, NE, serotonin
33
Q
  • What type of receptors do catecholamines activate? Biochemically speaking-what type of receptors are these?
A
  • Alpha and beta adrenergic (also DA)
  • GPCR
34
Q
  • What are the primary adrenergic receptors on the heart?
A

Beta 1

35
Q
  • What is the agonist for an alpha 1 adrenergic receptor?
  • What is it’s main G protein?
  • What tissue does it effect?
  • What effects does it cause?
A
  • Epinephrine
  • Gq (increase PLC,IP3, DAG)
  • Vascular, GU smooth muscle, heart, intestinal smooth muscle
  • Constriction
  • Increased contractile force in the heart
36
Q
  • What is the agonist for an apha 2 adrenergic receptor?
  • What G protein does it use?
  • What tissues does it effect?
  • What are the physiological effects?
A
  • Epinephrine more so than NE
  • Gi/G0 (Decrease adenylyl cyclase activity and lowers cAMP)
  • Platelets, nerve terminals, vascular smooth muscle, Beta cells of pancrease
  • Clotting, Constriction, Decreased insulin secretion
37
Q
  • What are the agonists for beta 1 adrenergic receptors?
  • What is its G protein?
  • What tissues does it affect?
  • What are the physiological responses?
A
  • EPI AND NE
  • Gs; increased adenylyl cyslase, cAMP, *L type Ca2+ channel opening*
  • Juxtaglomerular cells and heart
  • Increased renin secretion, increased force and rate of contraction, increased AV nodal conduction velocity
38
Q
  • What are the agonists for a beta 2 adrenergic receptor?
  • What is its G protein?
  • What tissues does it affect?
  • What are the physiological responses?
A
  • Epi >> NE
  • Gs; increase in adenylyl cyclase
  • Smooth muscle, skeletal muscle
  • Dilation, glycogenolysis, uptake of K+
39
Q
  • What is the rule of thumb for alpha 1 receptors?
A

Stimulate contraction of all smooth muscle

Vasoconstriction in vascular smooth muscle

40
Q
  • What is the rule of thumb for beta 2 receptors?
A
  • Vasodilation
  • (I remeber when my beta died (beta receptor die-a-lates; LAME AS HELL BUT IF IT HELPS YOU REMEMBER?)
41
Q
  • What is the rule of thumb for muscarinic receptors?
A
  • Contract smooth muscle (with a different intracellular signaling pathway than alpha 1 receptors)
42
Q
  • What is the response of sympathetic nervous system on the SA node?
  • What receptor is responsible for this physiologic response?
A
  • Increases heart rate
  • Beta 1
43
Q
  • What is the result of sympathetic activity on the atria?
  • What adrenergic receptor is responsible for this effect?
A
  • Increased contractility and conduction velocity
  • B1
44
Q
  • What is the result of sympathetic stimulation of the AV node/ His Purkinje System?
  • What receptor is responsible?
A
  • Increase in automaticity and conduction velocity
  • B1
45
Q

What is the result of sympathetic activation of the ventricles?

What adrenergic receptor is responsible?

A

Increased contractility, conduction velocity, automaticity and rate of idioventricular pacemakers

B1

46
Q
  • What is the result of sympathetic activation of arteries and arterioles?
  • What receptors are responsible?
A
  • Constriction
  • Alpha 1
47
Q
  • What is the result of sympathetic activation of tracheal and bronchial smooth muscle? What about bronchial glands?
  • What receptors are responsible for these effects?
A
  • Relaxation, decreased secretion (alpha 1), increased secretion (beta 2)
  • Beta 2, alpha 1, alpha 2
48
Q
  • What effect does parasympathetic activation have on the heart?
  • What receptors are responsible for this effect?
A
  • Decrease in HR
  • M2 receptors
49
Q
  • What affect does parasympathetic stimulation have on the atria?
  • What receptors are involved?
A
  • Decrease in contractility and shortened AP duration
  • M2
50
Q

What effect does parasympathetic stimulation have on the AV node and His/Purkinje System?

What receptors are involved?

A
  • Decrease in conduction velocity, AV block, little effect
  • M2
51
Q
  • What effect does parasympathetic stimulation have on the ventricles?
  • What receptors are involved?
A
  • Slight decrease in contractility
  • M2
52
Q
  • Where in the body is there no parasympathetic innervation?
A
  • Arteries and arterioles
53
Q
  • What effect does parasympathetic stimulation have on the endothelium of blood vessels?
  • What receptors are involved?
A
  • Activation of NO synthase
  • M3
54
Q
  • What effect does parasympathetic stimulation have on tracheal/bronchial smooth muscle and bronchial glands?
  • What receptors are involved?
A
  • Contraction, stimulation
  • M2,M3
55
Q
  • What is another name for EDRF?
A

NO

56
Q
  • What type of ANS innervation innervates the adrenal medulla?
  • What triggers the release of Epi and NE from adrenal medulla?
  • What is the ratio of NE/Epi released?
A
  • Sympathetic
  • Release of ACh from preganglionic fibers
  • ACh binds NAChRs and produces a localized depolarization
  • Release is 80% epi, 20% NE
57
Q
  • What happens as a respone of stretch in baroreceptors?
  • What drug elicits this stretching?
A
  • Parasympathetic activation
  • Phelylephrine