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Pharmacology - Principles > Autonomic Nervous System 2 > Flashcards

Autonomic Nervous System 2 Flashcards

0
Q

What do Presynaptic Autoreceptors do in the Parasympathetic System?

A

They mediate Negative Feeback Inhibition.

This limits the amount of ACh produced

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1
Q

What does a Beta 1 and a Gs protein receptor stimulate in the Sympathetic Nervous System?

A

Causes Stimulation of Adeylycyclcase

Increases the rate and the force of the Heart

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2
Q

What do Presynaptic Autoreceptors do in the Sympathetic System?

A

Act as a part of the Negative Feedback system

Detects the amount of NA in the synaptic cleft

If too much, limits the amount of Ca2+ entering the pre-ganglionic cell

Therefore limits the amount of NA being exocytosed into the synaptic celft

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3
Q

What effect does cocaine have on the Autonomic Nervous System?

A

Cocaine blocks the U1 uptake system.

This causes NA to accumulate in the synaptic cleft

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4
Q

What are Nicotinic Acetylcholine Receptors made of?

A

Consists of five glycoprotein subunits

  • There are many variations
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5
Q

What are the proteins that are used to assemble a Nicotinic Receptor?

A 
Alpha 1 to Alpha 10 
Beta 1 to Beta 4 
Gamma 
Sigma 
Epsilon
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6
Q

In a ganglionic Nicotinic Receptor were are the binding sites?

A

They are found between the Beta and Alpha subunits

  • There are two binding sites for the ligand.
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7
Q

What are the ions that enter and leave the Nicotinic Receptors?

A

Na+
K+
Ca 2+

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8
Q

What ion/ions move into the cell?

A

Sodium

Calcium

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9
Q

What ion/ions move out of the cell?

A

Potassium

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10
Q

Describe Cholinergic Transmission.

A
  1. Choline taken up via the transporter
  2. Choline and Acetate Co A synthesised to Acetyl Choline (ACh)
  3. ACh is stored in vesicles
  4. Depolarisation by action potential causes opening of voltage activated Calcium channels.
  5. Calcium induces the ACh to exocytose
  6. ACh binds to Nicotinic and Muscarinic Receptors activating them
  7. ACh broken down by acetylcholinesterase
  8. Choline taken back up
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11
Q

What is ACh synthesised from?

A

Acetyl-Co A

Choline

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12
Q

What is the ion that causes ACh vesicles exocytosis into the synaptic cleft in Cholinergic Transmission?

A

Calcium

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13
Q

What is the enzyme that breaks ACh down, after activating the receptors on the post-synaptic cell?

A

acetylcholinesterase (AChE) – terminates transmission

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14
Q

Describe cholinergic transmission at the ganglia

A
  1. ACh exocytoses from pre-ganglionic terminals
  2. ACh binds to the receptors causing the
    nicotinic ACh receptors to open
  3. Na+ then flows into the Post-ganglionic
    dendritic body
  4. This creates a small graded depolarisation (it
    is also called an excitatory post synaptic
    potential) - amplitude of this response is
    variable - depends on amount of ACh
  5. E.P.S if big enough allow voltage activated
    ion channels to open
  6. This creates a small current that flows to Voltage activated Na+ channels
  7. The Na+ channels open allowing more sodium to enter
  8. This produces an Action Potential
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15
Q

What drug can act in the same manner as ACh?

A

Nicotine

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16
Q

In ganglia transmission what drug can selective block the receptors?

A

Hexamethonium

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17
Q

How does hexamethonium block the receptor?

A

Open channel block

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18
Q

What type of anatagonism is an open channel block?

A

Non-competitive antagonism

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19
Q

Describe Cholinergic transmission at a Parasympathetic Neuroeffector Junction?

A

For the parasympathetic system it requires stimulation
of Muscarinic ACh receptors 1, 2 and 3

Otherwise same as general transmission

20
Q

What G Protein is associated with an M1 receptor in the parasympathetic system?

A

Gq

21
Q

What does stimulation of the M1/Gq muscarinic receptor in the parasympathetic system cause?

A

Stimulation of Phospholipase C

Acts on the stomach

Increased Acid Secretion

22
Q

What G Protein is associated with M2 muscarinic Receptor in the parasympathetic system??

A

Gi

23
Q

What does stimulation of the M2/Gi muscarinic receptor in the parasympathetic system cause?

A

Inhibition of adenylyl cyclase; opening of K+ channels

Decreased heart rate

24
Q

What G Protein is associated with an M3in the parasympathetic system?

A

Gq

25
Q

What does stimulation of the M3/Gq muscarinic receptor cause in the parasympathetic system?

A

Stimulation of phospholipase C

Increased Secretion of Saliva

Contraction of smooth muscles of the lungs

26
Q

Describe Noradrenergic transmission at Sympathetic Junctions.

A
  1. Synthesis of NA
  2. Storage of NA by transporter (concentrates)
  3. Depolarization by action potential
  4. Ca2+ influx through voltage-activated Ca2+ channels
  5. Calcium induced release of NA.
  6. Activation of adrenoreceptors
  7. Reuptake of NA via U1 or U2
  8. Metabolism of NA by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT)
27
Q

What is the enzyme that breaks NA down in the Pre-ganglionic neurone (U1) ?

A

monoamine oxidase (MAO)

28
Q

What is the enzyme that breaks NA down in the Post-ganglionic neurone U2?

A

catechol-O-methyltransferase (COMT)

29
Q

What is Emma Box ?

A

Metabolised ACh that has been forgotten about and never to be used ever again.

JOKES!

30
Q

What is the G protein associated with a Beta 1 Receptor in the Sympathetic System?

A

Gs

31
Q

What is the G protein associated with a Beta 2 Receptor in the Sympathetic System?

A

Gs

32
Q

What is the G protein associated with an Alpha 1 Receptor in the Sympathetic System?

A

Gq

33
Q

What is the G protein associated with an Alpha 2 Receptor in the Sympathetic System?

A

Gi

34
Q

What does activation of the B1/Gs receptor cause?

A

Stimulation of adenylyl cyclase

Increased rate and force of heart

35
Q

What does activation of the B2/Gs receptor cause?

A

Stimulation of adenylyl cyclase

Relaxation of bronchial and vascular smooth muscle

36
Q

What does activation of the A1/Gq receptor cause?

A

Stimulation of phospholipase C

Contraction of vascular smooth muscle

37
Q

What does activation of the Alpha 2/ Gi receptor cause?

A

Inhibition of adenylyl cyclase

Inhibition of NA release

38
Q

How does a Nerve Terminal of Post-ganglionic Parasympathetic Neurone
mediate negative feedback?

A

There is an Muscarinic 2 Autoreceptor on the Presynaptic cell that detects the amount of Ach

39
Q

How does a nerve Terminal of Post-ganglionic Sympathetic Neurone mediate negative feedback?

A

There is an Alpha 2 Muscarinic receptor on the presynaptic cell that detects the amount of Na

40
Q

What decreases the amount of neurotransmitter in the synaptic cleft?

A

An agonist

41
Q

What increases the amount of neurotransmitter in the synaptic cleft?

A

An antagonist

42
Q

What affect does cocaine have on the autonomic nervous system?

A

Affects the sympathetic system

Blocks U1 increasing the concentration of NA in the synaptic cleft resulting in increased adrenoceptor stimulation

43
Q

What affect does cocaine and amphetamine have on the peripheral actions of the body?

A

Causes Vasoconstriction and Cardiac Arrhythmias

44
Q

What affect does Amphetamine have on the autonomic nervous system?

A

Affects the Sympathetic System

  1. Amphetamine is a substrate for U1
  2. Enters the noradrenergic terminal where it inhibits MAO
  3. Displaces NA into the synaptic cleft
  4. Noradrenaline exits the terminal on U1
  5. NA accumulates in the synaptic cleft causing increased adrenoceptor stimulation
45
Q

What affect does Prazosin have on the body?

A

Selective, competitive, antagonist of alpha 1. Does not block alpha 2, beta 1, or beta 2. Vasodilator used as an anti-hypertensive agent

46
Q

What affect does Atenolol have on the body?

A

Selective, competitive, antagonist of Beta 1. Does not block Beta 2, Alpha 1, or Alpha 2. Used as an anti-anginal and anti-hypertensive agent

47
Q

What affect does Salbutamol have on the body?

A

Selective agonist at Bea 2. Does not activate, Beta 2, Alpha 1, or Alpha 2. Used as a bronchodilator in asthma

48
Q

What is Atropine’s affect on the body?

A

It is a competitive antagonist of muscarinic receptors

Blocks all muscarinic ACh receptors with equal affinity

Pharmacology - Principles (6 decks)

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