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Drugs: From molecule to man > Lecture 2: Autonomic Nervous System > Flashcards

Lecture 2: Autonomic Nervous System Flashcards

1
Q

What components does the preganglionic fiber link?

A

CNS to ganglion

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2
Q

What components does the postganglionic fiber connect?

A

Ganglion to gland cells, smooth muscle cells and cardiac muscle cells

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3
Q

Where does the output leave the spinal cord in the parasympathetic division?

A

At cranial and sacral regions

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4
Q

Where does the output leave the spinal cord in the sympathetic division?

A

It runs all the way down the spinal cord

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5
Q

What is the structure of acetylcholine?

A

Has a permanent positive charge
Has ester linkage

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6
Q

What are the two types of acetylcholine receptor?

A

Nicotinic and muscarinic

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7
Q

What are some features of nicotinic receptors?

A
  • Pentameric
  • 16 subunits
  • Many subtypes
  • Built in ion channels
  • 2+ ACh sites
  • Responses µs-ms
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8
Q

What are some features of muscarinic receptors?

A
  • Monomeric
  • M1-5 subtypes
  • 5 Receptor types
  • Binding site for G proteins
  • 1 ACh site
  • Responses ms-s
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9
Q

What are the agonists of nitotinic receptors?

A

Nicotine and Suxamethonium

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10
Q

What are the antagonists of nicotinic receptors?

A

Atracurium and tubocurarine

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11
Q

What are the agonists of muscarinic receptors?

A

Muscarine and Pilocarpine

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12
Q

What are the antagonists of muscarinic receptors?

A

Atropine and Hyosine

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13
Q

What is the process of the cholinergic terminal?

A
  1. Signal activates voltage gated calcium ion channels to open
  2. Calcium enters pre synaptic terminal
  3. Vesicles containing ACh fuse with membrane
  4. ACh diffuses across membrane and interacts with receptors
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14
Q

What is the processing of recycling choline?

A
  1. Leftover choline is taken back up to the nerve terminal by a carrier
  2. Its made back into ACh by enzyme choline acetyl transferase
  3. New ACh put into vesicles ready for release
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15
Q

Which parts of the nervous system are nicotinic receptors associated with?

A

NMJ, CNS and Autonomic ganglia

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16
Q

Which parts of the nervous system are the muscarinic receptors associated with?

A

CNS, Parasympathetic and Sympathetic

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17
Q

What are the different subtypes of muscarinic receptors?

A

M1 M2 M3 M4 M5

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18
Q

What is the location of M1?

A

Glands
Cerebral cortex
Autonomic ganglia

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19
Q

What is the pathway of M1?

A

IP3 (Gq)

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20
Q

What are the selected roles of M1?

A

Cognition (not fully known)

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21
Q

What are the therapeutic targets of M1?

A

Schizophrenia, Alzeimer’s and Cancer

22
Q

What are the side effects of M1?

A

Cognitive issues

23
Q

What are the locations of M2?

A

Heart, CNS and smooth muscle

24
Q

What is the pathway of M2?

A

↓cAMP (Gi)

25
Q

What are the selected roles of M2?

A

Modulate heart rate, Modulate smooth muscle

26
Q

What are the therapeutic targets of M2?

A

Bradycardia, Alzheimer’s, Depression

27
Q

What are the side effects of M2?

A

Tachycardia

28
Q

What are the locations of M3?

A

Glands, smooth muscle

29
Q

What is the pathway of M3?

30
Q

What are the selected roles of M3?

A

Smooth muscle contraction and exocrine secretion

31
Q

What are the therapeutic targets of M3?

A

Overactive bladder
IBS
Siogren’s syndrome
Glaucoma

32
Q

What are the side effects of M3?

A

Dry mouth
Constipation
Worse glaucoma
T2DM

33
Q

What are the locations of M4?

A

CNS and salivary gland

34
Q

What is the pathway of M4?

A

↓cAMP (Gi)

35
Q

What are the selected roles of M4?

A

Salivary gland (not fully known)

36
Q

What are the therapeutic targets of M4?

A

Drug addiction

37
Q

What are the side effects of M4?

A

Hypersalivation

38
Q

What is the location of M5?

39
Q

What is the pathway of M5?

40
Q

What are the selected roles of M5?

41
Q

What are the therapeutic targets of M5?

A

Drug addiction

42
Q

What are the side effects of M5?

43
Q

What are selective ligands?

A

Agonist binding site is highly conserved
Very few selective agonists or competitive antagonists

44
Q

What are the agonists of Adrenaline?

A

Adrenaline and noradrenaline

45
Q

What is the difference between adrenaline and noradrenaline?

A

Adrenaline has an extra methyl group on the nitrogen
Both are catecholamines

46
Q

What is the process of adrenaline at the synapse?

A
  1. NT interacts with adrenoreceptor GPCR
  2. NT not broke down but reuptaken whole into synapse and surrounding cells
  3. Amount of NT in vesicles controlled by enzymes
47
Q

What is the process of the biosynthesis of adrenaline?

A
  1. Tryosine becomes L-DOPA using tyrosine hydroxylase
  2. L-DOPA becomes Dopamine using DOPA decarboxylase
  3. Dopamine becomes Noradrenaline using Dopamine B(eta)-hydroxylase
  4. Noradrenaline becomes Adrenaline using Phenylethanolamine N-methyltransferase
48
Q

How many adrenergic neurons and receptors are in the sympathetic and central nervous system?

A

All 9 subtypes

49
Q

What is alpha 1?

A

Andrenoceptor
Does vasoconstriction
Contracts visceral smooth muscle
Relaxes GI tract
Agonist = Phenylephrine
Antagonist = Doxazosin

50
Q

What is beta 1?

A

Adrenoceptor
Increases heart rate and contraction force
Release of renin
Agonist = Dobutamine
Antagonist = Atenolol

51
Q

What is beta 2?

A

Andrenoceptor
Bronchodilation
Vasodilation
Relax smooth muscle
Agonist = Salbutamol and salmeterol
Antagonist = Butoxamine

Drugs: From molecule to man (21 decks)

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