Intro to Autonomic Pharm

Question 1

The ANS is not influenced by voluntary control and it regulates:

Answer 1

• contraction and relaxation of smooth muscle
• all exocrine and certain endocrine secretions
• heartbeat
• certain steps in intermediary metabolism

Question 2

In the heart the CNS/PNS dominates

Answer 2

PNS (parasympathetic nervous system)

Question 3

The control of blood pressure is mainly sympathetic/parasympathetic

Answer 3

Sympathetic

Question 4

Sweat glands, kidney and the adrenal medulla are innervated only by _________

Answer 4

Sympathetic

Question 5

What are the cholinergic fibers?

Answer 5

• ALL preganglionic autonomic fibers
• all parasympathetic post ganglionic fibers
• all somatic motor fibers to skeletal muscle

Question 6

Example of a sympathetic chilinergic fiber?

Answer 6

Sweat glands; they are sympathetic fibers that release acetylcholine

Question 7

The ______________ fibers in the kidney release ____________ that act on the renal vascular smooth muscle

Answer 7

Sympathetic; dopamine

Question 8

What is the rate limiting step in the synthesis of acetylcholine?

Answer 8

Bringing in choline into the neuron via the CHT1 transporter that also requires sodium (symport)

Question 9

M2 muscarinic receptor is found on __________________ and is ___________

Answer 9

Presynaptic neuron; inhibitory in action by binding and inactivating acetylcholine

Question 10

Where is dopamine converted into NE?

Answer 10

Inside the vesicle

Question 11

The α 2 adrenergic receptor on the _________ neuron causes ________

Answer 11

Presynaptic;

↓ further release of NE

Question 12

What are the two types of cholinergic receptors?

Answer 12

• nicotinic (ion channel linked) : neuronal and muscle type

- muscarinic (G protein linked)

Question 13

Neuronal nicotinic receptors are found on ________

Answer 13

Plasma membranes of the cell bodies of POST ganglionic parasympathetic and sympathetic receptors

Question 14

Where can muscarinic receptors be found?

Answer 14

• organs innervated by parasympathetic nerves
• can be found in tissues that are NOT innervated by parasympathetic nerves BUT have these receptors but can get activate (endothelial cells)
• tissues innervated by cholinergic postganglionic nerves (sweat glands which are sympathetic)

Question 15

Where can M1 receptors be found and what are the effects

Answer 15

• ganglia, CNS and vomiting center

- causes: depolarization, ↑ cognitive function, and emesis

Question 16

Where can M2 receptors be found and what are the effects?

Answer 16

• heart (atria), presynaptic Nerve terminal s

- cardiac inhibition and inhibition of acetylcholine release

Question 17

Where are M3 receptors located and what are the effects

Answer 17

• smooth muscles, secretory glands, vascular endothelium
• contraction of smooth muscle
• secretion
• vasodilation of vascular endothelium (only receptors are found here)

Question 18

Endothelial cells that line blood vessels have uninnervated M3 receptors contain the enzyme __________ which catalyzes: _________

Answer 18

NO synthase; formation of NO from arginine

Question 19

What is the effect of NO on the smooth muscle cells?

Answer 19

NO activates guanylyl sh last which causes the formation of cGMP from GTP
- cGMP activates a kinase which then phosphorylates proteins → relaxation of smooth muscle → vasodilation

Question 20

All___________ receptors are G protein coupled receptors

Answer 20

Adrenergic

Question 21

All β adrenergic receptors activate __________ via interaction with ______

Answer 21

Adenylyl cyclase; Gs

Question 22

_______ and_______ of the β adrenergic receptors have equal affinity for _________ and ______

Answer 22

β1 and β3; NE and epinephrine

Question 23

β2 has higher affinity for ________

Answer 23

epinephrine

Question 24

Tissues with ________ receptors such as the vasculature of skeletal muscle are responsive to circulating ____________ released by the adrenal medulla

Answer 24

Β2; epinephrine

Question 25

Where are α1 and β1 receptors found and what is the importance of their location

Answer 25

Found near the adrenergic nerve terminals so they can be activated when the nerves are stimulated

Question 26

Where are α2 and β2 receptors located? What is the effect of their location on their activation?

Answer 26

- Located at sites remote form the nerve terminals | - they are activated preferentially by circulating epinephrine

Question 27

Α2 and β2 receptors are activated preferentially by __________

Answer 27

Circulating epinephrine

Question 28

What it the signaling method of β1 receptors?

Answer 28

↑ cAMP; Gs

Question 29

What are the specific locations of the β1 receptor

Answer 29

- heart - Juxtaglomerular (JG) cells - adipocytes

Question 30

What are the effects on the heart when the β1 receptors are activated?

Answer 30

↑ Heart rate ↑ Heart force ↑ AV conduction velocity

Question 31

What is the effect on the JG cells when the _____ receptors are activated

Answer 31

β1; | ↑ renin release

Question 32

What is the effect of β1 receptor activation on adipocytes?

Answer 32

↑ lipolysis

Question 33

What is the effect on the activation of ______ receptors on the pancreatic cells?

Answer 33

β2; - pancreatic β cells: ↑ insulin secretion - pancreatic α cells: ↑ glucagon secretion

Question 34

Where can you find β2 receptors? (6)

Answer 34

- smooth muscle - skeletal muscle - pancreatic α cells - pancreatic β cells - liver - adipocytes

Question 35

What is the effect of activation of β2 receptors on skeletal muscle?

Answer 35

↑ glycogenolysis | ↑ K+ uptake

Question 36

What is the signaling mechanism of β receptors?

Answer 36

Gs coupled; ↑ cAMP etc

Question 37

What is the signaling mechanism for α1 receptors and where are they located?

Answer 37

↑ IP3 and DAG ↑ Calcium; Gq Located at: vascular and genitourinary SM and the liver

Question 38

What is the effect of α1 receptors at the smooth muscles?

Answer 38

Vascular and genitourinary SM → contraction

Question 39

What is the signaling mechanism for α2 receptors?

Answer 39

↓ cAMP through Gi → inhibition of NE release, inhibition of lipolysis

Question 40

What is the effect of α2 receptors on platelets, pancreatic ____ cells and the vascular smooth muscle?

Answer 40

- platelet aggregation - ↓ insulin secretion - contraction

Question 41

Where can the α2 receptors be found?

Answer 41

- presynaptic nerve terminals - platelets - adipocytes - pancreatic β cells - vascular SM

Question 42

____ and _____ receptors act on the pancreatic β cells but _____ has more power and leads to a net effect of _____

Answer 42

α2 and β2 receptors; | α2 has more effect leading to an over effect of ↓ insulin secretion

Question 43

What do you have more of in the vascular smooth muscle: α1 or α2 receptors?

Answer 43

α1

Question 44

Dopamine receptors are predominately found in _______________ causing _________

Answer 44

Smooth muscle of renal vascular bed; relaxation and thus improving blood flow to the kidney

Question 45

The receptor found in the salivary glands are ______

Answer 45

Parasympathetic cholinergic M3 receptors

Question 46

The primary controlled variable in the cardiovascular function is the __________

Answer 46

Mean arterial pressure

Question 47

What is the net effect of NE on the heart when accounting of the negative feed back baroeceptor response (homeostasis)?

Answer 47

- ↑ peripheral vascular resistance (contraction of SM) - moderate ↑ in MAP - BRADYCARDIA (opposite of drugs direct action)

Question 48

The cells of the medulla are modified __________ ___________ neurons

Answer 48

Post ganglionic sympathetic

Question 49

Describe the uniqueness of the innervation of sweat glands

Answer 49

They have sympathetic fibers that release acetylcholine and act on muscarinic receptors (all other post ganglionic sympathetic fibers act on either α or β adrenoreceptors aka they are noradrenergic and act by releasing NE)

Question 50

Dopamine is released by some peripheral _________ fibers

Answer 50

Sympathetic

Question 51

What is the enzyme that synthesizes acetylcholine from acetyl CoA and choline?

Answer 51

Choline acetyltransferase (ChAT)

Question 52

Synthesis of all catecholamines in the nervous systems originates from the amino acid ____________

Answer 52

Tyrosine

Question 53

What is the rate limiting step in the creating of dopamine?

Answer 53

Tyrosine → L-DOPA which is done by the enzyme tyrosine hydroxylase

Question 54

________ receptor actuation are response for the vagal inhibition fo the heart and the CNS and periphery

Answer 54

M2

Question 55

________ activates endothelial nitric oxide synthase leading to the formation of NO from _________

Answer 55

Calcium; | Arginine

Question 56

How does the release of NO lead to vasodilation?

Answer 56

NO binds to and activates guanylyl cyclase which catalyzes the formation of cGMP which ten acres the cGMP dependent protein kinase → phosphorylates proteins → vasodilation

Question 57

NE stimulates renin secretion by directly acting on juxtaglomerular cells of the kidney as is mediated by _________ receptors

Answer 57

β1 adrenergic receptors