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Neuropharmacology > Receptors and Subunits > Flashcards

Receptors and Subunits Flashcards

1
Q

How many subunits make up an AMPA receptor?

A

4

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2
Q

What are the different types of AMPA receptor subunits?

A

GluA1, GluA2, GluA3, GluA4

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3
Q

Which subunit of AMPAR determines low calcium permeability? Why is this?

A

GluA2 (which most AMPAR have) - because positive arginine is expressed instead of neutral glutamine.

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4
Q

Is AMPAR inotropic or metabotropic?

A

It is an ionotropic non-selective cation channel (so sodium ions in, potassium ions out)

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5
Q

What type of receptors are Kainate receptors?

A

Ionotropic

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6
Q

How many subunits for Kainate receptors have?

A

4

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7
Q

What are the possible subunits in a Kainate receptor?

A

GluK1, GluK2, GluK3, GluK4 and GluK5

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8
Q

Which Kainate receptor subunits do not form functional receptors when expressed alone?

A

GluK4 and GluK5

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9
Q

What does the Q/R site in Kainate receptors determine?

A

GluK1 and GluK2’s permeability for calcium ions.

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10
Q

Which subunit is necessary for Kainate receptors to make an excitatory postsynaptic response?

A

GluK2

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11
Q

What are the names of NMDA receptor subunits?

A

GluN1, GluN2A, GluN2B, GluN2C, GluN2D, GluN3A and GluN3B

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12
Q

NMDA receptors are heterotetramers of what?

A

Two GluN1 (NR1) subunits and two GluN2 (NR2) subunits

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13
Q

Which section of the NMDA receptor is the glycine binding site in?

A

NR1

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14
Q

Which section of the NMDA receptor is the glutamate binding site in?

A

NR2

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15
Q

Which receptor has the ‘Mg2+ block’?

A

NMDA receptors

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16
Q

What type of receptors are NMDA receptors?

A

Ionotropic

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17
Q

Which metabotropic glutamate receptors are part of Group 1, what type of GPCR are they and how do they signal?

A

mGlu1 and mGlu5

Galphaq signalling leading to increased phospholipase C, increased IP3 and increased calcium ion concentration.

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18
Q

Which metabotropic glutamate receptors are part of Group 2, what type of GPCR are they and how do they signal?

A

mGlu2 and mGlu3
Galphai/o, leading to decrease in activation of andenylyl cyclase and consequently cAMP and decreased calcium ion concentration.

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19
Q

Which metabotropic glutamate receptors are part of Group 3, what type of GPCR are they and how do they signal?

A

mGlu4, mGlu6, mGlu7 and mGlu8
Galphai/o leading to decrease in activation of andenylyl cyclase and consequently cAMP and decreased calcium ion concentration.

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20
Q

Which postsynaptic metabotropic glutamate receptors mediate slow depolarisation?

A

mGlu1 and mGlu5 (aka Group 1)

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21
Q

Which groups of presynaptic metabotropic glutamate receptors decrease neurotransmitter release?

A

Group 2 and Group 3

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22
Q

What type of receptors are Glycine receptors?

A

Ionotropic

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23
Q

How many subunits are Glycine receptors comprised of?

A

5

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24
Q

What type of receptors are GABA-A receptors?

A

Ionotropic

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25
Q

What is the most common combination of subunits of GABA-A receptors in the mammalian brain?

A

1 x alpha, 2 x beta and 2 x gamma

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26
Q

How many subunits create a GABA-A receptor?

A

5

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27
Q

Benzodiazepines do not work on GABA-A receptors containing which subunits?

A

Alpha 4 and/or alpha 6

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28
Q

What are names of the possible GABA A subunits?

A

Alpha1-6, Beta1-3, Gamma1-3, Delta, Epsilon, Pi, Theta and Rho1-3

29
Q

What subunits are most GABA A receptors comprised of?

A

2 Alpha, 2 Beta and 1 Gamma/1 Delta

30
Q

Where do benzodiazepines bind to on the GABA A receptor?

A

The alpha gamma subunit interface

31
Q

What type of receptors are GABA B receptors?

A

GPCR/Metabotropic

32
Q

What type of GPCR is a GABA B receptor? What are the downstream effects of binding?

A

Galphai/o - they are negatively couple to adenlyl cyclase leading to inhibition of cAMP production, activated GIRK potassium channels and inhibits voltage sensitive calcium channels.

33
Q

What is the molecular target of the Group 1 anaesthetics (e.g. Etomidate, Propofol and Pentobarbitol)?

A

GABA A Receptor

34
Q

The presence of which GABA A receptor subunit abolishes potentiation of the IV anaesthetic Etomidate?

A

Beta3

35
Q

A mutation in which GABA A receptor subunit reduces the hypnotic response and abolishes the immobility response to Etomidate and Propofol?

A

Beta3

36
Q

Group 2 anaesthetics (e.g. Nitrous Oxide, ketamine, xenon and cyclopropane) act on which molecular targets?

A

NMDA receptors, AMPA receptors, neuronal ACh receptosrs and 2 pore potassium channels.

37
Q

Group 3 anaesthetics (the halogenated ethers and alkanes, such as isofluorane and halothane) act on which molecular targets?

A

GABA A receptors, glycine receptors, NMDA receptors, AMPA receptors, neuronal ACh receptors and 2 pore potassium channels.

38
Q

Anaesthetic potency of propofol correlates with its ability to…?

A

Potentiate GABA A receptor mediated chloride currents.

39
Q

Hypnosis and amnesia in anaesthesia is due to potentiation of which receptor?

A

GABA A receptor

40
Q

Immobilisation in anaesthesia is mediated by potentiation of which receptor?

A

Glycine receptor

41
Q

Inhibition of which receptor leads to analgesia during anaesthesia?

A

NMDA receptors

42
Q

What two receptors have other unspecified contribution to anaesthetic effects?

A

Neuronal ACh receptors and potassium channels.

43
Q

Which receptor is in both the sympathetic and parasympathetic autonomic nervous systems?

A

Nicotinic cholinergic receptors

44
Q

Which type of receptor is only present in the sympathetic section of the autonomic nervous system?

A

Adrenergic receptors

45
Q

Which type of receptor is only present in the parasympathetic section of the autonomic nervous system?

A

Muscarinic receptors

46
Q

What are the different isoforms of muscarinic receptors in the parasympathetic nervous system and how do they signal?

A

M1, M3 and M5 - stimulate phospholipase C

M2 and M4 - inhibit adenlyl cyclase

47
Q

What are the different isoforms of adrenergic receptors in the sympathetic nervous system and how do they signal?

A

Alpha1 - activates phospholipase C
Alpha2 - Inhibits adenlyl cyclase
Beta1, Beta,2 and Beta3 - Increase cAMP

48
Q

What are the different types of dopamine receptor and how do they signal?

A

D1-like (D1 and D5) - GalphaS - increases cAMP

D2-like (D2, D3 and D4) - Galphai - decreases cAMP

49
Q

Which dopamine receptor can be an autoreceptor?

A

D2

50
Q

Which 5-HT receptor’s a Galphai/o leading to decreased cAMP?

A

5HT1A, 5HT1B, 5HT1D, 5HT1E and 5HT1F

51
Q

Which 5HT receptor is a ligand gated ion channel?

A

5HT3

52
Q

Which 5HT receptor is GalphaS that is implicated in learning and memory?

A

5HT6

53
Q

Which 5HT receptor is implicated in modulation of exploratory behaviour? What type of GPCR is it?

A

5HT5A - GalphaS

54
Q

5HT4 is which type of GPCR?

A

GalphaS

55
Q

Which serotonin receptor is an inhibitory presynaptic receptor that becomes desensitised after chronic SSRI treatment?

A

5HT1A receptor

56
Q

Which serotonin receptors are Galphaq, therefore leading to increased DAG and IP3?

A

5HT2A, 5HT2B and 5HT2c

57
Q

LSD is mainly an agonist of which receptor?

A

5HT2A receptor

58
Q

Psilobycin is an agonist of 5HT2AR but also has high affinity for which receptors?

A

5HT2B and 5HT2C

59
Q

Which agonism of which serotonin receptor is necessary for the effects of ‘classic’ hallucinogens?

A

5HT2A receptors

60
Q

Which receptor does cortisol behind to?

A

Glucocorticoid receptors

61
Q

What does activation of glucocorticoid receptors lead to in glutamatergic synapses?

A

Induces glutamate release, endocannabinoid production and can exacerbate glutamate induced excitotoxicity.

62
Q

Which cannabinoid receptor is expressed in the brain, lungs and liver?

A

CB1 receptor

63
Q

What type of GPCR is CB1? What effect does it have?

A

Galphai/o - positively regulates GIRK channels, negatively regulates calcium channels and inhibits adenlyl cyclase leading to decreased cAMP

64
Q

Is CB1 pre or postsynaptic?

A

Presynaptic

65
Q

What type of GPCR are all opioid receptors?

A

Galphai/o

66
Q

How do opioids suppress pain?

A

Act as presynaptic receptor e.g. mu opioid receptor suppresses calcium channel opening, reducing synaptic transmission and therefore reducing transmission of pain signals up to sensory cortex.

67
Q

What type of GPCR is A1 Receptor?

A

Galphai/o - decreases cAMP

68
Q

What type of GPCR is A2A receptor?

A

GalphaS - increasing cAMP leading to increased GABA release

Neuropharmacology (15 decks)

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