3 - Monoamines Flashcards

(49 cards)

1
Q

What is the chemical definition of a monoamine

A

A neurotransmitter containing one amino group connected to an aromatic ring by a two-carbon chain

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2
Q

What cognitive processes do monoamines regulate (3)

A

Emotion
Arousal
Certain types of memory

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3
Q

What are monoamines synthesised from

A

Decarboxylated amino acids

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4
Q

What is synthesis of monoamines catalysed by

A

Cytosolic enzymes

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5
Q

What receptors do monoamines usually activate

A

GPCR

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6
Q

Is synthesis of monoamines limited to certain regions of the brain

A

Yes

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7
Q

What are the 5 steps involved with monoamine release at the synapse

A
  1. Synthesis
  2. Storage
  3. Release
  4. Receptor action
  5. Inactivation
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8
Q

What is the synthesis pathway of the catecholamines

A
  1. L-tyrosine
  2. L-DOPA
  3. Dopamine
  4. Noradrenaline
  5. Adrenaline
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9
Q

What is the enzyme that turns L-tyrosine to L-DOPA

A

Tyrosine hydroxylase

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10
Q

What is the enzyme that turns L-DOPA into dopamine

A

Aromatic L-amino acid decarboxylase

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11
Q

What is the enzyme that turns dopamine into noradrenaline

A

Dopamine B-hydroxylase

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12
Q

What enzyme turns noradrenaline into adrenaline

A

Phenylethanolamine N-methyl-transferase

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13
Q

What is the synthesis pathway for the indoleamines

A

L-tryptophan
5-hydroxy-L-tryptophan
5-hydroxytryptamine

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14
Q

What is the enzyme that converts Tryptophan to 5-HTP

A

Typtophan hydroxylase

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15
Q

What is the enzyme that converts 5-HTP to 5-HT

A

Aromatic L-amino acid decarboxylase

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16
Q

What increases 5-HT synthesis

A

Dietary tryptophan

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17
Q

What is L-DOPA used to treat

A

Parkinson’s Disease

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18
Q

What is 5-HTP used to treat

A

Depression, anxiety and insomnia

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19
Q

How are monoamines stored in the synapse (4)

A

Bound complex with ATP, protein, Ca and Mg

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20
Q

What transports monoamines into the vesicles

21
Q

Which amphetamines are substrates for VMAT (3)

A

MDMA, dexamphetamine, methamphetamine

22
Q

What is the MOA of amphetamies

A

Compete with monoamines for vesicular storage

Increase cytoplasmic monoamine increases spontaneous leakage into the synapse

23
Q

What CNS diseases are due to DA storage and release issues

A

Substance use disorder
Parkinson’s Disease
Schizophrenia

24
Q

Which monoamines are dysregulated in depression

25
Are D1 receptors excitatory or inhibitory
Excitatory | Vice versa for D2
26
Which dopamine receptors are D1-like
D1, D5
27
Which dopamine receptors are D2-like
D2, D3, D4
28
What is the adrenoceptor hierarchy for adrenaline
B2 > B1/B3/a
29
What is the adrenoceptor heirarchy for noradrenaline
a > B1 >> B2
30
Which 5HT receptor is ionotropic
5HT3
31
Which 5HT receptor mediates inhibition
5HT1
32
How are serotonin receptors classified (3)
Clonal sequence Signal transduction mechanisms Pharmacological specificity
33
How are monoamines reuptaken from the synapse (3)
Active transport via high affinity Na dependent membrane transporter proteins: DAT, NAT, SERT
34
How does cocaine work
Blocks NAT, SERT and DAT
35
How do amphetamines work
Compete with monoamines at DAT, NAT, SERT
36
How to tricyclic antidepressants work
Block NAT, SERT > DAT
37
How do noradrenaline reuptake inhibitors work
Block NAT
38
How do SNRI work
SERT, NAT
39
How do SSRIs work
SERT
40
How does bupropion work
Atypical antidepressant, blocks NAT, DAT. Promotes release of NA, DA (NDRA). Anti-nicotinic. Many metabolites
41
How are monoamines broken down
MAO via oxidative deamination
42
What does MAO-A degrade
5-HT NA A DA
43
What does MAO-B degrade
DA
44
What is dopamine broken down into
Homovanillic acid
45
What is noradenaline broken down into
Vanillylmandelic acid
46
What are the two enzymes involved in 5-HT breakdown
MAO | Aldehyde dehydrogenase
47
What is a MAO-B inhibitor used in the treatment of Parkinson's Disease
Selegiline
48
What CNS functions and diseases are monoamines involved in (9)
``` Mood Anxiety Schizophrenia Reward Drug abuse Movement Pain Regulation of autonomic function Regulation of hormone release ```
49
What are the four dopamine pathways
Tubero-infundibular Nigrostriatal Mesocortical Mesolimbic