Lecture 10 (DSA): Intro to ANS Pharm

Question 1

How do agonists activate a receptor?

Answer 1

Activate the receptor to signal as a direct result of binding to it.

Question 2

Agonists can activate a receptor to produce effects in what 2 ways?

Answer 2

1) All of the receptors biologic functions

2) Selectively promote one function more than another

Question 3

Antagonists do what to the signaling of receptor?

Answer 3

Block the generation of a signal by binding to the receptor

Question 4

What are cholinomimetic agents?

Answer 4

Drugs that mimic ACh:

• AChR agonists
• Acetylcholinesterase inhibitors

Question 5

What are cholinoceptor-blocking drugs?

Answer 5

AChR antagonists

Question 6

What are sympathomimetic agents?

Answer 6

Drugs that mimic or enhance α- and β- receptor (agonists)

Question 7

What are 2 ways sympathomimetic agents act as an agonist?

Answer 7

1) Enhance catecholamine release

2) Block re-uptake of catecholamines

Question 8

What are adrenoceptor-blocking drugs?

Answer 8

α- and β- receptor antagonists

Question 9

How does sympathetic innervation of the SA node affect heart rate?

Answer 9

Increases heart rate

Question 10

What is the receptor on the SA node for sympathetic innervation?

Answer 10

β1 adrenergic receptor

Question 11

How does parasympathetic innervation of the SA node affect heart rate?

Answer 11

Decrease in heart rate

Question 12

What is the receptor on the SA node for parasympathetic innervation?

Answer 12

M2 (muscarinic)

Question 13

What does sympathetic innervation of the atria cause?

Answer 13

Increase in contractility and conduction velocity?

Question 14

What is the receptor in the atria for sympathetic innervation?

Answer 14

β1 adrenergic receptor

Question 15

What does parasympathetic innervation of the atria cause?

Answer 15

Decrease in contractility

Question 16

What is the receptor in the atria for parasympathetic innervation?

Answer 16

M2 (muscarinic)

Question 17

What does sympathetic innervation of the tracheal and bronchial smooth muscle cause?

Answer 17

Relaxation

Question 18

What is the primary receptor for sympathetic innervation of the bronchial and tracheal smooth muscle?

Answer 18

β2 adrenergic receptor

Question 19

What does parasympathetic innervation of the tracheal and bronchial smooth muscle cause?

Answer 19

Contraction

Question 20

What is the primary receptor for parasympathetic innervation of the bronchial and tracheal smooth muscle?

Answer 20

M2=M3 (muscarinic)

Question 21

What does sympathetic innervation of the bronchial glands cause?

Answer 21

Decreased secretion or increased secretion

Question 22

What are the α1 receptors of bronchial glands responsible for?

Answer 22

Decreased secretion

Question 23

What are the β2 receptors of bronchial glands responsible for?

Answer 23

Increased secretion

Question 24

What does parasympathetic innervation of the bronchial glands cause?

Answer 24

Contraction

Question 25

What receptors are found on bronchial glands for parasympathetic innervation?

Answer 25

M2, M3 (muscarinic)

Question 26

What are the neurotransmitters and receptors for parasympathetic nervous system?

Answer 26

NT: ACh Receptors: nAChR and mAChR

Question 27

What are the neurotransmitters and receptors for sympathetic nervous system?

Answer 27

NE > Epi; ACh Receptors: α, β, nAChR, and mAChR

Question 28

Sympathetic nervous system uses what NT to activate which receptor in the adrenal medulla to release what NT?

Answer 28

ACh activates nicotinic ACh receptors to release epinephrine

Question 29

Sweat glands contain what receptor on them and are innervated by what part of the autonomic NS?

Answer 29

Muscarininc choline receptos (mAChR) activated by ACh from the sympathetic nervous system

Question 30

Synthesis of epinephrine primarily occurs where; from what?

Answer 30

Adrenal medualla from NE---->Epi

Question 31

Dopamine is the precursor to what?

Answer 31

NE and epinephrine

Question 32

Which muscarinic receptors are coupled to Gq/11 and their activation results in?

Answer 32

M1, M3, M5 - Activation of PLC; IP3, DAG cascade (smooth muscle contraction)

Question 33

When IP3 levels go up what occurs?

Answer 33

Contraction of smooth muscle

Question 34

Which muscarinic receptors are coupled to Gi/o and their activation results in?

Answer 34

M2 and M4 - Inhibition of AC; decreased cAMP production, activation of K+ channels

Question 35

A decrease in cAMP production controlled by the M2 receptors of cardiac muscle have what affect?

Answer 35

Decrease in strength and force of contraction in cardiac tissue, decreases rate.

Question 36

Why is having M3 receptors important in the gut?

Answer 36

When stimulated by the parasympathetic nervous system will causes contraction allowing for digestion to resume

Question 37

Explain the basic mechanism of tyrosine to NE?

Answer 37

Tyrosine enters the nerve and is converted to dopa, then to dopamine (in the cytoplasm). Dopamine is shuttled into vesicle where it is converted to NE.

Question 38

After the NE or epi has performed its function on the α- or β-receptors what occurs?

Answer 38

Will undergo reuptake by a transporter and be stored until needed again.

Question 39

What is the vesicular monoamine transporter (VMAT-2)?

Answer 39

- Transports NE, Epi, DA, and serotonin into vesicles for storage - Inhibited by Reserpine

Question 40

What does cocaine inhibit?

Answer 40

Blocks the transporter of NE, causes NE accumulation

Question 41

What are the 2 main enzymes for the metabolism of catecholamines?

Answer 41

1) Monoamine oxidase (MAO) | 2) Catechol-O-methyltransferase (COMT)

Question 42

Are there degradative enzyme for catecholamines during signaling?

Answer 42

No, they differ from cholinergic signaling, and instead undergo reuptake into the nerve.

Question 43

Where are the Alpha-1 receptors found?

Answer 43

Vascular, GU smooth muscle, intestinal smooth muscle, Heart

Question 44

What is the Alpha-1 response in the vascular and GU smooth muscle?

Answer 44

Contraction = Vasoconstriction

Question 45

What is the Alpha-1 response in the heart?

Answer 45

Increased contractile force, arrhythmia's

Question 46

Where are the Alpha-2 receptors found?

Answer 46

Vascular smooth muscle, pancreatic islet (B cells), Platelets, and nerve terminals

Question 47

Function of Alpha-2 receptors in nerve terminals and vascular smooth muscle?

Answer 47

Nerve terminals - Decreased release of NE Vascular - Contraction

Question 48

Function of Alpha-2 receptors on platelets?

Answer 48

Aggregation

Question 49

Where are the Beta-1 receptors found?

Answer 49

Heart and Juxtaglomerular cells

Question 50

Function of the Beta-1 cells in the heart?

Answer 50

Increased force and rate of contraction and AV nodal conduction velocity

Question 51

Where are the Beta-2 receptors found?

Answer 51

Smooth muscle (vascular, bronchial, GI, GU), Skeletal muscle

Question 52

Function of Beta-2 receptors

Answer 52

- Relaxation of smooth muscle | - Glycogenolysis; uptake of K+

Question 53

Epinephrine has a stronger affect on which adrenergic receptor?

Answer 53

Beta-2

Question 54

In the heart which receptor produces the greatest sympathetic effects?

Answer 54

Beta-1

Question 55

In the blood vessels which receptor predominates for the sympathetic nervous system?

Answer 55

Alpha-1

Question 56

In the heart which receptor predominates for parasympathetic innervation?

Answer 56

Muscarinic (M2)

Question 57

In the blood vessels which receptor predominates for parasympathetic innervation?

Answer 57

Muscarinic (M3)

Question 58

ACh & muscarinic agonists given IV cause what, due to?

Answer 58

Vasodilation due to release of nitric oxide (NO)

Question 59

Smooth muscle of blood vessels are NOT innervated by?

Answer 59

Parasympathetic neurons

Question 60

Activation of mAChRs on endothelial cells causes production and release of?

Answer 60

Endothelium-derived relaxing factor (EDRF), also known as nitric oxide (NO)

Question 61

Where are chromaffin cells located and what kind of receptor do they contain?

Answer 61

Found within the Adrenal Medulla and contain NAChR's

Question 62

What are the effects of Reserpine?

Answer 62

Blockade of NE storage and depletion by MAO

Question 63

Botulinum toxin effects?

Answer 63

Anticholinergic; inhibition of NT release

Question 64

Nicotine and pilocarpine are?

Answer 64

nAChR and mAChR agonists (Cholinomimetic)

Question 65

Tubocurarine and atropine are?

Answer 65

nAChR and mAChR antagonists (Anticholinergic)

Question 66

Alpha blockers (phentolamine) and beta blockers (propranolol) are?

Answer 66

Antiadrenergic

Question 67

Alpha agonists (nepinephrine) and beta agonists (albuterol) are?

Answer 67

Adrenomimetic