Metabotrophic glutamate Flashcards
what family of GPCR are mGlu
Family 3
What rceptors are group 1 connected to
Gq
What subtypes are in group 1
mGlu1
mGlu5
What are group 2 coupled to
Gi
What are group 3 coupled to
Gi
What are in group 2
mGlu2
mGlu3
What are in group 3
mGlu4
mGlu6
mGlu7
mGlu8
What subtype are retinal
mGlu6
What is the structure of mGlu
Homo or heterodimers, containing a disulphide bond between the dimers
What is the binding required
Need a glutamate into both venus fly trap domains. They then close, changing the shape to activate the G protein
Agonists (2)
Glutamate
ACPD
Antagonist
MCPG - bulkier, stops closing
Group 1 location
Postsynaptically. Excitatory increasing Ca
Group 2/3 location
Presynaptically. Reduce excitation
What does ACPD cause presynatpically
Blocks EPSP
Postsynaptically, what channels does ACPD block
K channels
Where are mGluR1 located at glutaminergic synapses
Perisynaptically, can remove glutamate
How can mGlu mediate disinhibition
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
How can pain be reduced by mGlu
Use a group 1 antagonist to reduce wind up
What mGlu allosteric modulator can be used for parkinsons in rats and what R
PhCCC, agonist on mGlu4
what does PhCCC do
reduces reserpine induced akinesia in rats and protects against MPTP induced toxicity by reducing inhibitory pathway
In Fragile X sydrome, what gene is distrupted
FMR1
In FXS, what is association with mGlu
Hyperactive mGlu5
mGlu5 antagonist
mavoglurant
