Cholinergic Neurotransmitters Flashcards

1
Q

What channel is nicotinic receptor

A

Ion gated channel

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2
Q

What channel is muscarinic receptors

A

G protein coupled receptor

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3
Q

Which muscarinic receptors are inhibitory and which excitatory

A

1, 3, 5 - excitatory
2, 4 - inhibitory

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4
Q

What is G protein and its types

A

Guanine nucleotide-binding proteins
Gs
Gi
Go
Gq

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5
Q

Explain all the G protein types

A
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6
Q

What is the place of nicotinic ach receptors

A
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7
Q

What does muscarinic Ach receptors produce

A

Parasympathetic nerve effects in the heart, smooth muscles, and glands

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8
Q

Drugs affecting the PNS are useful for what

A
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9
Q

Neurons that release acetylcholine are what

A

Cholinergic

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10
Q

cholinergic agonists are called

A

Parasympathomimetics

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11
Q

Cholinergic antagonists are called

A

Parasympatholytics

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12
Q

Explain the structure of acetylcholine and why you can’t take it orally

A
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13
Q

Explain the biosynthesis of acetylcholine

A
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14
Q

What inhibits acetylcholine esterase

A

Phosphorus compounds

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15
Q

Why can’t we use acetylcholine as agonist

A

Flexible
Nonselective
Polar will not cross the membrane

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16
Q

Muscadine mimics what

A

The action of Ach

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17
Q

Where can you find M 2 and M3

A

Peripheral autonomic tissues

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18
Q

Where can you find M1 and M4

A

Brain and autonomic ganglia

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19
Q

With what does the M1 3 5 interact with

A
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20
Q

With what do M2 4 interact with

A
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21
Q

What are the advantages of acetylcholine

A

Natural messenger
Easily synthesized

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22
Q

What are the disadvantages of acetylcholine

A
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23
Q

What are the requirements for cholinergic agonists

A
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24
Q

Explain the acetylcholine in the muscarinic binding site

A
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25
Q

Summarize the SAR of acetylcholine

A
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26
Q

Explain the active conformation of acetylcholine

A
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27
Q

Explain the rigid analogues of acetylcholine

A
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28
Q

Explain choline ester

A
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29
Q

How to make choline ester have stability against hydrolysis

A
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30
Q

What is a disadvantage of carbachol and how to solve it

A
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31
Q

Explain the design of bethanechol

A
32
Q

Explain pilocarpine

A
33
Q

List the biological responses of cholinomimetics

A
34
Q

What is the clinical use of muscarinic cholinergic agonists

A
35
Q

What is the clinical use of nicotinic cholinergic agents

A
36
Q

Explain cholinergic agonist

A
37
Q

What is anti-cholinesterase

A
38
Q

How fast is Ach hydrolyzed

A
39
Q

AchE inhibitors are what

A

Indirect cholinomimetics

40
Q

What are the two main classes of AchE inhibitors

A

Carbamates
Organophosphorus compounds

41
Q

What is the normal mechanism of AchE

A
42
Q

Explain the reversible AchE inhibitor

A
43
Q

Give example of carbamates

A
44
Q

What is the clinical use of physostigmine

A
45
Q

Explain neostigmine and pyridostigmine

A
46
Q

What is the difference between physostigmine and neostigmine, pyridostigmine

A
47
Q

Explain the irreversible AchE inhibitor

A
48
Q

How to treat organophosphate compounds poisoning

A
49
Q

Explain nicotinic agonist

A
50
Q

Nicotinic agonists are used in treatment of what

A
51
Q

Explain cholinolytics

A
52
Q

What is the clinical use of muscarinic antagonists

A
53
Q

List the muscarinic antagonists

A

Atropine
Hyoscine
Atropine methonitrate
Ipratropium

54
Q

Explains Atropine

A
55
Q

What is the clinical use of atropine

A
56
Q

What is the contraindication of atropine

A

Glaucoma

57
Q

How to make Ach antagonist

A

Add aromatic ring in the ester group

58
Q

Explain Hyoscine and its use

A
59
Q

What is a similarity between atropine and Hyoscine

A
60
Q

Compare between atropine and Ach

A
61
Q

Explain Atropine Methonitrate and its use

A
62
Q

Explain Ipratropium and its use

A
63
Q

Explain Tiotropium bromide and its uses

A
64
Q

Explain the SAR for antagonists

A
65
Q

What are the two types of nicotinic antagonists

A

Ganglionic blocking agent
Skeletal neuromuscular blocking agent

66
Q

Explain ganglionic blocking agent

A
67
Q

Explain skeletal neuromuscular blocking agents

A
68
Q

List neuromuscular blocking agents

A

Curare
Decamethonium
Suxamethonium
Atracurium
Snake toxin

69
Q

Explain curare

A
70
Q

What is the clinical use of curare

A
71
Q

Explain decamethonium

A
72
Q

Explain Suxamethonium

A
73
Q

Explain Atracurium

A
74
Q

Explain mecamylamine

A
75
Q

What is mecamylamine used for

A
76
Q

Explain Snake toxin

A