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Pharm 2A > Receptors Masterlist > Flashcards

Receptors Masterlist Flashcards

1
Q

What are the 3 ionotropic (S)-Glutamate receptors

A

NMDA, AMPA, Kainate

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2
Q

How many types of metabotropic Glutamate receptors are there

A

8

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3
Q

What are the Group 1 metabotropic glutamate receptors

A

mGlu1 and 5

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4
Q

What G protein is coupled to Group 1 metabotropic glutamate receptors

A

G(alphaq)

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5
Q

What are the Group 2 metabotropic glutamate receptors

A

mGlu2 and 3

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6
Q

What G protein is coupled to Group 2 metabotropic glutamate receptors

A

G(alphai/o)

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7
Q

What are the Group 3 metabotropic glutamate receptors

A

mGlu4, 6, 7, 8

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8
Q

What G protein is coupled to Group 3 metabotropic glutamate receptors

A

G(alphai/o)

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9
Q

Where are ionotropic glutamate receptors located

A

post-synaptic

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10
Q

How many subunits make up the ionotropic glutamate receptors

A

4 - tetrameric assembly

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11
Q

What are the subunits in an AMPAR

A

GluA1-4

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12
Q

What is the make-up of an AMPAR

A

receptors can form homomers or heteromers

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13
Q

What are the subunits in a Kainate receptor

A

GluK1-5

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14
Q

What is the make-up of Kainic receptors

A

GluK1-3 can form homomers. GluK4 and GluK5 can only form functional receptors as heteromers with GluK1-3

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15
Q

Which receptor contains a Q/R site

A

AMPARs

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16
Q

What is the Q/R site responsible for

A

Modulating receptor permeability to calcium and sodium ions

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17
Q

Under what conditions is an AMPAR permeable to calcium and sodium ions

A

When glutamine is bound to the receptor

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18
Q

Under what conditions is an AMPAR not permeable to ions

A

When arginine is bound to the receptor

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19
Q

Where is the amino terminal domain located

A

extracellular

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20
Q

Where is the carboxy terminal domain located

A

intracellular

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21
Q

What does the amino terminal domain contain

A

Negative allosteric modulator binding site

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22
Q

What are the subunits in NMDARs

A

GluN1 and GluN2A-D

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23
Q

What is the most common make-up of NMDARs

A

2xGluN1 + 2xGluN2

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24
Q

What are the 3 important properties of NMDARs

A
  1. highly permeable to calcium ions
  2. channel blocked by magnesium ions
  3. glycine is a necessary co-agonist with glutamate
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25
Q

What are the conditions for NMDA channel blocking

A

Mg2+ can only block the channel when both glutamate and glycine are bound

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26
Q

How is NMDA channel blocking released

A

AMPA activation

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27
Q

Where does glycine bind on the NMDAR

A

GluN2

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28
Q

Where does glutamate bind on NMDARs

A

GluN1

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29
Q

What is an example of a negative allosteric modulator which binds to NMDARs

A

eliprodil - anticonvulsant

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30
Q

Where is site C located in the NMDAR

A

in the transmembrane domain

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31
Q

What is site C in the NMDAR

A

channel blocker binding site

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32
Q

What is the role of NMDARs

A

mediate slow excitatory post-synaptic response via calcium and sodium entry

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33
Q

What are the 2 types of GABA receptors

A

GABAA and GABAB

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34
Q

What type of receptor is GABAA

A

ligand-gated ion channel

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35
Q

What does GABAA do when activated

A

allows entry of chloride ions into neurones

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36
Q

Where are GABAA receptors located

A

post-synaptic

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37
Q

How many subunits do GABAA receptors have

A

5 - pentameric

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38
Q

What are all the different subunits of GABAA receptors

A

6alpha, 3beta and 3gamma

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39
Q

What is the most common combination of GABAA receptors

A

2alpha, 2beta and 1gamma

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40
Q

What binds to the alpha-beta interface in the GABAA receptor

A

GABA agonists and competitive antagonists

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41
Q

Where do benzodiazepines bind on the GABAA receptor

A

alpha-gamma interface

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42
Q

What other compounds bind at the GABAA receptor

A

barbiturates. general anaesthetics, neurosteroids, ethanol

43
Q

What blocks the GABAA channel pore

A

Picrotoxin

44
Q

What are the subunits of GABAB receptors

A

GABAB1 and GABAB2

45
Q

What type of G-protein is coupled to GABAB receptors

A

Gi/o

46
Q

What are the effects of GABAB receptor activation

A
  1. Increased K+ output
  2. Decreased Ca2+ uptake
  3. decreased cAMP -> increase PKA
47
Q

How does GABAB receptor activation affect transmitter release presynaptically

A

inhibiting voltage-gated calcium channels

48
Q

How does GABAB receptor activation affect postsynaptic excitability

A

reduces postsynaptic excitability by increasing potassium output

49
Q

What receptor does noradrenaline bind to

A

alpha and beta adrenoceptors

50
Q

What are the subtypes of receptors which noradrenaline act on

A

alpha1, 2 and beta1-4

51
Q

What beta-adrenoceptors are present in the CNS

A

beta 1 and 2

52
Q

Are adrenoceptors ionotropic or metabotropic

A

metabotropic

53
Q

What G-protein is coupled to alpha1-adrenoceptors

A

Gq

54
Q

What G-protein is coupled to alpha2-adrenoceptors

A

Gi/o

55
Q

What G-protein is coupled to beta-adrenoceptors

A

Gs

56
Q

Where are alpha1-adrenoceptors located

A

post-synaptic

57
Q

Where are alpha2-adrenoceptors located

A

pre and post-synaptic

58
Q

Where are beta-adrenoceptors located

A

pre and post-synaptic

59
Q

What are the 2 receptor families that are acted on by dopamine

A

D1 and D2

60
Q

Are dopamine receptors ionotropic or metabotropic

A

metabotropic

61
Q

What receptors are included in the D1 family of dopamine receptors

A

D1 and D5

62
Q

What receptors are included in the D2 family of dopamine receptors

A

D2, 3 and 4

63
Q

Where are D1-family dopamine receptors located

A

post-synaptic

64
Q

Where are D2-family dopamine receptors located

A

pre and post-synaptic

65
Q

How many serotonin receptor subtypes are there

A

7

66
Q

Which 5-HT receptors are metabotropic

A

5-HT1, 2, 4-7

67
Q

Which 5-HT receptors are ionotropic

A

5-HT3

68
Q

What G-protein is coupled to 5-HT1 receptors

A

Gi/o

69
Q

What G-protein is coupled to 5-HT2 receptors

A

Gq

70
Q

Where and how do 5-HT1 receptors act

A

pre and post-synaptic inhibition

71
Q

Where and how do 5-HT2 receptors act

A

post-synaptic excitation

72
Q

Where do 5-HT3 receptors act

A

post-synaptic

73
Q

Where do 5-HT4-7 receptors act

A

post-synaptic

74
Q

What does 5-HT1 receptor activation affect

A

mood (A)

75
Q

What does 5-HT2 receptor activation affect

A

behaviour (A/C), sleep, mood, anxiety

76
Q

What does 5-HT3 receptor activation affect

A

anti-emetic, mood, anxiety, nausea

77
Q

What are the 2 types of cholinergic receptors

A

nicotinic and muscarinic

78
Q

How many subunits are in a nicotinic acetylcholine receptor

A

5 - pentameric

79
Q

Are nAChRs ionotropic or metabotropic

A

ionotropic

80
Q

What are the nAChR subunits

A

alpha2-7, alpha9, alpha10, beta2-4

81
Q

What is the most common assembly of heteromeric nAChRs

A

2alpha4 + 3beta2

82
Q

What is the most common assembly of homomeric nAChRs

A

alpha7

83
Q

What are the effects of nAChRs

A

mediate effects of nicotine including arousal, enhanced learning and memory

84
Q

Are mAChRs ionotropic or metabotropic

A

metabotropic

85
Q

What are the main excitatory mAChR subtypes

A

M1, 3 and 5 (M1 family)

86
Q

What G-protein is coupled to the M1 family of mAChRs

A

Gq

87
Q

What are the effects of M1 family mAChR activation

A

activation leads to excitation through modulation of M-type K+ channels

88
Q

What are the inhibitory subtypes of mAChRs

A

M2 and M4

89
Q

What G-protein is coupled to M2 and M4 mAChRs

A

Gi/o

90
Q

What are the 5 classical opioid receptors

A

mu, delta, kappa, ORL1 and nociceptin

91
Q

Are opioid receptor ionotropic or metabotropic

A

metabotropic

92
Q

What G-protein is coupled to opioid receptors

A

Gi/o

93
Q

What are the presynaptic effects of opioid receptor activation

A

inhibit transmitter (glutamate and substance P) release through inhibition of calcium channels

94
Q

What are the postsynaptic effects of opioid receptor activation

A

inhibit neuronal firing through activation of potassium channels

95
Q

How do opioid receptors cause excitation

A

disinhibition in the ventral tegmental area (VTA) -> enhances dopamine release in the nucleus accumbens

96
Q

What are the main effects of mu opioid receptor activation

A

analgesia, euphoria, respiratory depression, constipation

97
Q

What are the main effects of delta opioid receptor activation

A

analgesia, dysphoria, diuresis

98
Q

What are the main effects of kappa opioid receptor activation

A

analgesia, antidepressant, proconvulsant

99
Q

What are the Cannabinoid receptor subtypes

A

CB1 and CB2

100
Q

Are cannabinoid receptors ionotropic or metabotropic

A

metabotropic

101
Q

What G-protein is coupled to cannabinoid receptors

A

Gi/o

102
Q

Where are CB1 receptors located

A

high expression in CNS, high density in cortex and basal ganglia

103
Q

Where are CB2 receptors located

A

lymphoid tissue, immune cells

Pharm 2A (10 decks)

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