Recceptors Flashcards

1
Q

GPCR’s

A

G-protein coupled receptors
Gs and Gq are excitatory recepetors
Gi is an inhibitatory receptor

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2
Q

Ionotropic

A

Ligand gated ion channels
Multi-subunit and heterogenous
Rapid cellular effects
Affects pharmacology and pharmacology

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3
Q

Metabotropic

A
GPCR's 
Can be homo/heterodimers
Slower and more diffuse response involved in neromodulation 
Can activate 2nd messenger systems 
Can also act as auto-receptors
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4
Q

Autoreceptors

A

A form of negative feedback where the neurotransmitter the receptor released can bind to that receptor and deactivate it preventing synaptic levels of that neurotransmitter getting too high.

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5
Q

GABAa receptors

A

Iontropic: Cl- channel
Fast acting and inhibitory
Can be targeted by agonist muscimole and antagonist biculline
GABA binds to orthosteric site

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6
Q

GABAb receptors

A

Metabotropic: heterodimer
Made up of R1 which has a venus fly trap GABA binding site while R2 traffics the receptor up to the surface

Closes Ca2+ channels presynaptically to reduce neurotransmitter release
Open K+ channels postsynaptically resulting in a slow hyperpolarisation

Targeted by GABAb agonist Baclofen

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7
Q

GABAc receptors

A

Ionotropic: Cl- channel
Fast inhibitory action
Targeted by agonist GABA/muscimol and antagonist TPMPA

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8
Q

NMDA recepetors

A

Ionotropic: Voltage gated Ca2+ ion channel
Usually blocked by Mg2+ but this block disappears when the cell is depolarised
Activation requires both glutamate and glycine
Antagonised by Ketamine/phenylcyclidine
Increases Glu release presynaptically via increasing Ca2+ influx

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9
Q

mGlu receptors

A

Metabotropic
Slow neuromodulatory role
Gp1 receptors found presynaptically, Gp2/3 are found post synaptically
Reduces glutamate release presynaptically by decreasing Ca2+ influx

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10
Q

VMAT

A

Vesicular mono amine transporter
Only present on vesicle membranes
Transports monoamines into vesicles for storage

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11
Q

COMT

A

Catechol O methyl transferase
Inactivates NA/DA
Overexpression of COMT is a phenotype for schizophrenia

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12
Q

MAO

A

Monoamine oxidase

Inactivates NA/DA/5HT

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13
Q

DAT

A

Dopamine transporter

Present on cell surface membrane for uptake of DA from synaptic cleft

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14
Q

NAT

A

Noradrenaline transporter

Present on cell surface membrane for uptake of NA from synaptic cleft

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15
Q

SERT

A

Serotonin transporter

Present on cell surface membrane for uptake of 5HT from synaptic cleft

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16
Q

5HT receptors

A

5HT1-7

5HT3 is ionotropic, rest are metabotropic

17
Q

NA receptors

A

Alpha 1/2 and Beta 1/2

18
Q

DA recepetors

A

D1-Gs coupled
D2-Gi-coupled
All are metabotropic

19
Q

ACh receptors

A

ACh acts on nicotinic (ionotropic) and muscarinic (metabotropic) receptors

20
Q

AChesterase

A

Acetylcholinesterase is the enzyme that inactivates ACh in the synpatic cleft to free choline and acetyl groups

21
Q

Histamine receptors

A

H1-4 are all GPCR’s

H1 receptors on C-fibres sensitise VR-1 nociceptors and respomds to histamine released by mast cells

22
Q

ASIC receptor

A

Acid sensing ion channel
Nociceptive receptor
Allows influx of Na+
Detects H+ ions at free nerve endings

23
Q

Purinergic receptors

A

Nociceptive receptor that detects ATP and high threshold mechanical stimulation (really hard hits)
Allows influx of Na+
Can also detect the ATP released by damaged cells

24
Q

Voltage gated Na+ channel (VGNa) (C-fibre associated)

A

Detects mechanical stimuli

Allows influx of Na+

25
Q

VR-1/TRPV-1/Vanilloid/Capsacin recepetor

A

Responds to H+ ions and heat
Also activated by capsacin
Opens to allow entry of Na+/Ca2+ and form graded potentials

26
Q

TrKA receptor

A

Responds to NGA (nerve growth factor)

Involved in nociceptor sensitisation via sensitising VGNa and VR-1 receptors

27
Q

Prostanoid receptors

A

Responds to prostaglandins

Involved in nociceptor sensitisation via sensitising BK1 and VGNa receptors

28
Q

BK2 receptors

A

Bradykinin receptor

Involved in nociceptor sensitisation via sensitising VR-1 receptors

29
Q

Mu opioid receptor

A

The only opioid receptor in the brain but also found along spine and periphery

Involved in analgesia, euphoria, respiratory depression and constipation

30
Q

Delta opioid receptor

A

Only found along the spine

Involved in analgesia, dysphoria and diuresis

31
Q

Kappa opioid receptor

A

Found along the spine and periphery

Invloved in analgesia and acts as a proconvulsant

32
Q

Features found in all opioid receptors

A

Gi coupled receptor
Opens Ca2+/Closes K+
Decreases conversion of AMP to cAMP therefore there is less PKA