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Neuropharm > Metabotrophic glutamate > Flashcards

Metabotrophic glutamate Flashcards

1
Q

what family of GPCR are mGlu

A

Family 3

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2
Q

What rceptors are group 1 connected to

A

Gq

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3
Q

What subtypes are in group 1

A

mGlu1

mGlu5

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4
Q

What are group 2 coupled to

A

Gi

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5
Q

What are group 3 coupled to

A

Gi

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6
Q

What are in group 2

A

mGlu2

mGlu3

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7
Q

What are in group 3

A

mGlu4
mGlu6
mGlu7
mGlu8

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8
Q

What subtype are retinal

A

mGlu6

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9
Q

What is the structure of mGlu

A

Homo or heterodimers, containing a disulphide bond between the dimers

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10
Q

What is the binding required

A

Need a glutamate into both venus fly trap domains. They then close, changing the shape to activate the G protein

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11
Q

Agonists (2)

A

Glutamate

ACPD

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12
Q

Antagonist

A

MCPG - bulkier, stops closing

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13
Q

Group 1 location

A

Postsynaptically. Excitatory increasing Ca

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14
Q

Group 2/3 location

A

Presynaptically. Reduce excitation

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15
Q

What does ACPD cause presynatpically

A

Blocks EPSP

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16
Q

Postsynaptically, what channels does ACPD block

A

K channels

17
Q

Where are mGluR1 located at glutaminergic synapses

A

Perisynaptically, can remove glutamate

18
Q

How can mGlu mediate disinhibition

A

Found on GABA releasing golgi cells. mGlu 2/3 reduce the release of GABA due to their inhibitory functions. TJis allows a bigger EPSP on granule cells by mossy fibres. Only atimulated after repeated firing of glu

19
Q

How can pain be reduced by mGlu

A

Use a group 1 antagonist to reduce wind up

20
Q

What mGlu allosteric modulator can be used for parkinsons in rats and what R

A

PhCCC, agonist on mGlu4

21
Q

what does PhCCC do

A

reduces reserpine induced akinesia in rats and protects against MPTP induced toxicity by reducing inhibitory pathway

22
Q

In Fragile X sydrome, what gene is distrupted

A

FMR1

23
Q

In FXS, what is association with mGlu

A

Hyperactive mGlu5

24
Q

mGlu5 antagonist

A

mavoglurant

Neuropharm (15 decks)

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