2.2 - CNS Drugs (General)

Question 1

Which two substances are combined by ChAT to produce ACh?

Answer 1

Choline + Acetyl CoA

Question 2

What is ChAT?

Answer 2

Choline Acetyl Transferase
–> The enzyme that converts choline and acetyl CoA to produce ACh.

Question 3

Which enzyme breaks down ACh within the synaptic cleft?

Answer 3

Acetylcholine esterase (AChE)

Question 4

AChE turns ACh into…

Answer 4

Choline (which is taken back up and made into more ACh), and acetate (Which enters the Krebs cycle)

Question 5

Which drug results in the inhibition of choline reuptake from synapse?

Answer 5

Hemicholinium
–> Decreased further synthesis of ACh

Question 6

What is hemicholinium?

Answer 6

A drug that inhibits choline reuptake within the synapse

Question 7

Which drugs inhibits ACh storage in the vesicle?

Answer 7

Vesamicol

Question 8

What does vesamicol do?

Answer 8

Inhibits ACh storage in vesicle.

Question 9

Which drug prevents ACh release?

Answer 9

Botulinum toxin

Question 10

What does the botulinum toxin do to the body?

Answer 10

Prevent ACh NT release, resulting in muscle paralysis.

Question 11

What drug displaces ACh from vesicles?

Answer 11

Latrotoxin - black widow venom

Question 12

What does black widow toxin do to the body?

Answer 12

Latrotoxin displaces ACh from vesicles, therefore preventing its release. Leading to muscle paralysis.

Question 13

What are the two kinds of cholinergic receptors?

Answer 13

Muscarinic and nicotinic

Question 14

Give an example of a PSNS cholinergic receptor agonist.

Answer 14

Muscarine

Question 15

Give an example of a PSNS cholinergic receptor antagonist.

Answer 15

Atropine

Question 16

What does muscarine do to the body?

Answer 16

Muscarinic cholinergic receptor agonist

Question 17

What does atropine do to the body?

Answer 17

Muscarinic receptor antagonist

Question 18

Which drug inhibits AChE?

Answer 18

Neostigmine, and nerve gases

Question 19

What is neostigmine?

Answer 19

AChE inhibitor - increases ACh levels by preventing is breakdown.

Question 20

All postganglionic receptors (of the neuron itself) in the ANS have which kind of ACh receptor?

Answer 20

Nicotinic

Question 21

Where are muscarinic receptors found in target tissue?

Answer 21

Smooth muscle and glands, sweat glands.

Question 22

All target tissue of the PSNS has which kind of cholinergic receptor?

Answer 22

Muscarinic (Smooth muscle and glands all have muscarinic ACh receptors)

Question 23

Where are nicotinic receptors found in the body?

Answer 23

On postganglionic neurons, skeletal muscle, and the adrenal medulla

Question 24

Where do SNS target tissues have muscarinic receptors?

Answer 24

In sweat glands

Question 25

What is a general rule for the roles of a1 receptors?

Answer 25

They are involves in vasoconstriction, or constriction

Question 26

What is the general rule for a2 receptors?

Answer 26

They are involved in negative feedback

Question 27

What is the general rule for B1 receptors?

Answer 27

The heart and kidneys

Question 27

What is the general rule for B2 receptors?

Answer 27

Relaxation/dilation

Question 28

Which two structures have B3 adrenergic receptors? What do they signal for?

Answer 28

Adipose tissue - lipolysis Bladder (detrusor) - Relaxation

Question 29

What kind of adrenergic receptors promote glycogenolysis and gluconeogenesis in the liver?

Answer 29

B2

Question 30

What kind of adrenergic receptors signal for decreased GI motility? What about GI secretions?

Answer 30

--> B2 for motility --> a2 for secretions

Question 31

What kind of adrenergic receptors signal for increased insulin secretion from the pancreas? What about decreased insulin secretion?

Answer 31

--> Increased is B2 --> Decreased is A2

Question 32

What kind of adrenergic receptors trigger for relaxation of the bronchi, uterus and bladder, as well as vasodilation near skeletal muscles and coronaries?

Answer 32

B2

Question 33

What kind of adrenergic receptors signal for increased heart rate and increased force of contraction?

Answer 33

B1

Question 34

What kind of adrenergic receptor signals for renin release on the kidneys?

Answer 34

B1

Question 35

What kind of adrenergic receptor signals for inhibition of NA release on presynaptic neurons?

Answer 35

a2

Question 36

What kind of adrenergic receptor signals for mydriasis, piloerector muscles, ejaculation, internal urinary sphincter contraction, and vasocontraction near the skin and splanchnic vessels?

Answer 36

a1

Question 37

What kind of adrenergic receptor signals for thick viscous secretions from the salivary glands?

Answer 37

A1

Question 38

Where are nicotinic neuronal receptors found? What does it do?

Answer 38

--> ANS postganglionic ganglions (complex and difficult to predict) --> Adrenal medulla (NE and E release at a 4:1 ratio)

Question 39

Where are nicotinic muscular receptors found?

Answer 39

Somatic skeletal muscles only. Leads to depolarization and contraction

Question 40

Which kind of cholinergic receptors are found in the brain?

Answer 40

M1, M4, M5.

Question 41

Where are M2 receptors found?

Answer 41

In the heart muscle - decreased heart rate, decreased force of atrial contraction

Question 42

Where are M3 receptors found? what do they do?

Answer 42

Smooth muscle and glands (Salivary, lacrimal, bronchial GI) Stimulates iris sphincter for miosis Contraction of ciliary muscle (accommodation) Sweat glands - diaphoresis (sympathetic)

Question 43

Which part of the SNS used cholinergic receptors? Which one does it use?

Answer 43

Sweat glands - M3