Synapse Flashcards
What does the ANS mainly regulate?
Contraction & Relaxation of smooth muscle
Exocrine systems
Heartbeat
Energy Metabolism
Which neurotransmitter regulates the sympathetic (fight or flight) nervous system?
Noradrenaline
Which neurotransmitter regulates the parasympathetic (rest or digest) nervous system?
Acetylcholine
Where does Acetylcholine (Ach) work?
Somatic NS
Parasympathetic NS
Limited Sympathetic NS
Where does Noradrenaline (NA) work?
Sympathetic NS
Where does Dopamine (DA) work?
CNS - Reward pathway
Where & how does Glutamate (GLU) work?
Main excitatory CNS neurotransmitter
Where & how does Gamma-amino butyric acid (GABA) work?
Main inhibitory CNS neurotransmitter
What does Serotonin control?
Sleep, Wakefulness & mood
What is Depolarisation & Repolarisation?
Depolarisation - influx of Na+ - towards Ena = + 60 mV
Repolarisation - Efflux of K+ - towards Ek = -84 mV
What happens when the neurotransmitter interacts with the Ionotropic receptor?
Activation causes influx of Na+ in post-synaptic terminal
Depolarisation occurs
AP is created (Signal propogation)
What happens when the neurotransmitter interacts with the Metabotropic receptor?
Triggers second messenger signalling cascades
Triggers functional responses ( e.g. muscle contraction)
How is further release of Ca2+ stopped?
When neurotransmitter reaches sufficient conc. in synaptic cleft
It activates pre-synaptic receptors
Sends negative signal into pre-synaptic terminal
Thus stopping further release of Ca2+
How is the signal terminated?
Reuptake of neurotransmitter into pre-synaptic terminal by use of monoamines
OR
Degradation of neurotransmitter in synaptic cleft by use of Acetylcholine
Which areas would be suitable for drug targeting in the synaptic transmission pathway?
- Synthesis
- Storage of neurotransmitter
- Neurotransmitter release
- Receptors
- Neurotransmitter termination
What are unprotected monoamines broken down by?
Monoamine Oxidase (MAO)
What is Reserpine’s MOA?
Prevents packaging monoamines into vesicles
Thus exposing them to MAO
What are ionotropic receptors?
Ligand-gated ion channels made up of many subunits
They mediate fast synaptic channels
What are Metabotropic receptors?
G protein coupled receptor (GPCR)
They mediate slower synaptic transmission - secondary messenger cascades
How are secondary messenger cascades initiated?
Agonist activates GPCR - causes a conformation change - exposes GDP/GTP exchange sites of G protein
Hydrolysis of GTP-GDP releases energy = which enables dissociation of alpha subunit from beta-gamma subunits
Which initiates secondary messenger cascades
What are the 3 main types of G proteins?
Gq - Stimulatory
Coupled to Phospholipase C
Gs - Stimulatory
Coupled to Adenylyl Cyclase
Gi- Inhibitory
Coupled to Adenylyl Cyclase
What class is Fluoxetine and what does it do?
Selective Serotonin Reuptake Inhibitors (SSRI)
Prolongs presence of Serotonin around post-synaptic receptors
by preventing reuptake of Serotonin
What drug class is Moclobemide and what does it do?
MAO inhibitor
Prolongs presence of Serotonin
by inhibiting Monoamine Oxidase A