Receptors Masterlist Flashcards by Jessica Loong

What are the 3 ionotropic (S)-Glutamate receptors

NMDA, AMPA, Kainate

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How many types of metabotropic Glutamate receptors are there

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What are the Group 1 metabotropic glutamate receptors

mGlu1 and 5

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What G protein is coupled to Group 1 metabotropic glutamate receptors

G(alphaq)

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What are the Group 2 metabotropic glutamate receptors

mGlu2 and 3

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What G protein is coupled to Group 2 metabotropic glutamate receptors

G(alphai/o)

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What are the Group 3 metabotropic glutamate receptors

mGlu4, 6, 7, 8

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What G protein is coupled to Group 3 metabotropic glutamate receptors

G(alphai/o)

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Where are ionotropic glutamate receptors located

post-synaptic

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How many subunits make up the ionotropic glutamate receptors

4 - tetrameric assembly

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What are the subunits in an AMPAR

GluA1-4

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What is the make-up of an AMPAR

receptors can form homomers or heteromers

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What are the subunits in a Kainate receptor

GluK1-5

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What is the make-up of Kainic receptors

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

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Which receptor contains a Q/R site

AMPARs

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What is the Q/R site responsible for

Modulating receptor permeability to calcium and sodium ions

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

When glutamine is bound to the receptor

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Under what conditions is an AMPAR not permeable to ions

When arginine is bound to the receptor

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Where is the amino terminal domain located

extracellular

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Where is the carboxy terminal domain located

intracellular

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What does the amino terminal domain contain

Negative allosteric modulator binding site

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What are the subunits in NMDARs

GluN1 and GluN2A-D

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What is the most common make-up of NMDARs

2xGluN1 + 2xGluN2

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What are the 3 important properties of NMDARs

highly permeable to calcium ions
channel blocked by magnesium ions
glycine is a necessary co-agonist with glutamate

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What are the conditions for NMDA channel blocking

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

How is NMDA channel blocking released

AMPA activation

Where does glycine bind on the NMDAR

GluN2

Where does glutamate bind on NMDARs

GluN1

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

eliprodil - anticonvulsant

Where is site C located in the NMDAR

in the transmembrane domain

What is site C in the NMDAR

channel blocker binding site

What is the role of NMDARs

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

What are the 2 types of GABA receptors

GABAA and GABAB

What type of receptor is GABAA

ligand-gated ion channel

What does GABAA do when activated

allows entry of chloride ions into neurones

Where are GABAA receptors located

post-synaptic

How many subunits do GABAA receptors have

5 - pentameric

What are all the different subunits of GABAA receptors

6alpha, 3beta and 3gamma

What is the most common combination of GABAA receptors

2alpha, 2beta and 1gamma

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

GABA agonists and competitive antagonists

Where do benzodiazepines bind on the GABAA receptor

alpha-gamma interface

What other compounds bind at the GABAA receptor

barbiturates. general anaesthetics, neurosteroids, ethanol

What blocks the GABAA channel pore

Picrotoxin

What are the subunits of GABAB receptors

GABAB1 and GABAB2

What type of G-protein is coupled to GABAB receptors

Gi/o

What are the effects of GABAB receptor activation

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

How does GABAB receptor activation affect transmitter release presynaptically

inhibiting voltage-gated calcium channels

How does GABAB receptor activation affect postsynaptic excitability

reduces postsynaptic excitability by increasing potassium output

What receptor does noradrenaline bind to

alpha and beta adrenoceptors

What are the subtypes of receptors which noradrenaline act on

alpha1, 2 and beta1-4

What beta-adrenoceptors are present in the CNS

beta 1 and 2

Are adrenoceptors ionotropic or metabotropic

metabotropic

What G-protein is coupled to alpha1-adrenoceptors

What G-protein is coupled to alpha2-adrenoceptors

Gi/o

What G-protein is coupled to beta-adrenoceptors

Where are alpha1-adrenoceptors located

post-synaptic

Where are alpha2-adrenoceptors located

pre and post-synaptic

Where are beta-adrenoceptors located

pre and post-synaptic

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

D1 and D2

Are dopamine receptors ionotropic or metabotropic

metabotropic

What receptors are included in the D1 family of dopamine receptors

D1 and D5

What receptors are included in the D2 family of dopamine receptors

D2, 3 and 4

Where are D1-family dopamine receptors located

post-synaptic

Where are D2-family dopamine receptors located

pre and post-synaptic

How many serotonin receptor subtypes are there

Which 5-HT receptors are metabotropic

5-HT1, 2, 4-7

Which 5-HT receptors are ionotropic

5-HT3

What G-protein is coupled to 5-HT1 receptors

Gi/o

What G-protein is coupled to 5-HT2 receptors

Where and how do 5-HT1 receptors act

pre and post-synaptic inhibition

Where and how do 5-HT2 receptors act

post-synaptic excitation

Where do 5-HT3 receptors act

post-synaptic

Where do 5-HT4-7 receptors act

post-synaptic

What does 5-HT1 receptor activation affect

mood (A)

What does 5-HT2 receptor activation affect

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

What does 5-HT3 receptor activation affect

anti-emetic, mood, anxiety, nausea

What are the 2 types of cholinergic receptors

nicotinic and muscarinic

How many subunits are in a nicotinic acetylcholine receptor

5 - pentameric

Are nAChRs ionotropic or metabotropic

ionotropic

What are the nAChR subunits

alpha2-7, alpha9, alpha10, beta2-4

What is the most common assembly of heteromeric nAChRs

2alpha4 + 3beta2

What is the most common assembly of homomeric nAChRs

alpha7

What are the effects of nAChRs

mediate effects of nicotine including arousal, enhanced learning and memory

Are mAChRs ionotropic or metabotropic

metabotropic

What are the main excitatory mAChR subtypes

M1, 3 and 5 (M1 family)

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

What are the effects of M1 family mAChR activation

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

What are the inhibitory subtypes of mAChRs

M2 and M4

What G-protein is coupled to M2 and M4 mAChRs

Gi/o

What are the 5 classical opioid receptors

mu, delta, kappa, ORL1 and nociceptin

Are opioid receptor ionotropic or metabotropic

metabotropic

What G-protein is coupled to opioid receptors

Gi/o

What are the presynaptic effects of opioid receptor activation

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

What are the postsynaptic effects of opioid receptor activation

inhibit neuronal firing through activation of potassium channels

How do opioid receptors cause excitation

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

What are the main effects of mu opioid receptor activation

analgesia, euphoria, respiratory depression, constipation

What are the main effects of delta opioid receptor activation

analgesia, dysphoria, diuresis

What are the main effects of kappa opioid receptor activation

analgesia, antidepressant, proconvulsant

What are the Cannabinoid receptor subtypes

CB1 and CB2

Are cannabinoid receptors ionotropic or metabotropic

metabotropic

What G-protein is coupled to cannabinoid receptors

Gi/o

Where are CB1 receptors located

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

Where are CB2 receptors located

lymphoid tissue, immune cells

Receptors Masterlist Flashcards

(103 cards)