GABA(A) Receptor Flashcards
GABA stands for?
Gamma amino butyric acid
GABA(A) receptor is a?
Heteropentamer
Most common GABA(A) receptor type
2alpha, 2beta, gamma
GABA(A) receptor agonists which compete for the same site
- GABA
- Baclofen
- Muscimol
GABA(A) receptor allosteric agonists
- Benzodiazepines
- Ethanol
- Barbiturates
- Avermectins
- Volatile anesthetics
- Some steroids
GABA(A) receptor antagonists
- Bicuculline
2. Some steroids
Mutations of the GABA(A) receptor are associated with?
Epilepsy and seizures
GABA(A) receptor inverse agonist
DMCM
What is an inverse agonist?
Binds to same receptor as agonist but produces opposite response
Gephryin is linked to?
- Tubules
- Profilin (actin)
- Collybistin
- Neuroglin 2
Collybistin is?
GTP exchange protein
Neuroligin 2 also interacts with?
Presynaptic neurexins
2 conditions associated with hyperekplexia
- Acoustic startle
2. Stiff baby
GABA and Glycine uptake/reuptake mechanisms are present in?
- Presynaptic nn.
2. Associated neuroglia
Glycine reuptake into presynaptic cell is regulated by what receptor?
GlyT2
Glycine reuptake into glial cell is regulated by what receptor?
GlyT1
GABA reuptake into glial cell is regulated by what receptor?
GAT3
How does glial cell recycle GABA?
Converts to gluamine
How does presynaptic neuron take up recycled glutamine?
SNAT1 or SNAT2
GABA reuptake into presynaptic cell is regulated by what?
GAT-1
Glycine has what efect on post-synaptic cell?
Inhibits
What hapens when glycine or GABA causes Cl- channels to open?
Hyperpolarizes cell
What type of inhibition can be overcome by increasing ligand concentration?
Competitive inhibition
GABA and glycine have what ultimate fate?
Reuptake
ACh has what ultimate fate?
Breakdown
Serotonin has what ultimate fate?
Breakdown or reuptake
ACh is broken down by?
Cholinesterase
Serotonin is broken down by?
Monoamine oxidase
Serotonin reuptake is modulated by what receptor?
SERTs
4 methods of response termination
- Dissociation
- Desensitization
- Down regulation
- Transmiter removal
3 methods of transmitter removal
- Breakdown/metabolism
- Diffusion from cleft
- Reuptake