Neurotransmitters Flashcards
A NT must be :
in presynaptic terminal
release in response to stimuli
interact on post synapotic receptor
be rapidly removed
Amin and AA nt are ….
The amino acid and amine neurotransmitters are:
small molecules
stored and released from synaptic vesicles
capable of many binding to and activating both
ligand-gated channel receptors
G-protein coupled receptors
Peptide nt are …
large molecules
stored in secretory granules
only activate G-protein coupled receptors
dales principle
A neuron only has one neurotransmitter’
Dale classified neurons into mutually exclusive groups by the neurotransmitter they released
glutamate ;
Most common excitatory transmitter in CNS
Amino acid, therefore, found in all neurons
3 glutamate receptor subtypes based on the drugs which act as selective agonists : NMDA,AMPA, kainate
Action is terminated by selective uptake into presynaptic terminals and glia
AMPA receptor
AMPA receptors mediate fast excitatory transmission.
Glutamate binding to AMPA receptors triggers Na+ and K+ currents resulting in an EPSP
NMDA receptor
- often co-exist with AMPA receptors
- have a voltage-dependent Mg2+ block. so therefore sodium cannot pass in. Need Vm to become more positive so Mg not as attracted and is removed so sodium and calcium can enter
- are permeable to Ca2+ as well as Na+ and K+
- Therefore their activation can have more widespread, lasting changes in the postsynaptic cell
GABA nt
Not an amino acid used to synthesise proteins
Precursor is glutamate
Synthesis requires the enzyme glutamic acid decarboxylase
inhibitory in CNS
GABA A receptor
is ionotropic
lets Cl- in to make more negative to suppress
can inactivtate Ca+ channels
GABA B receptor
GPCR
activate kinase
phosphorylate calcium channels
other chemicals that can bind to GABA a channels when GABA also binds
Ethanol has behavioural effects, addictive
Benzodiazepines e.g. diazepam, used to treat anxiety
Barbiturates are sedatives and anti-convulsants
Neurosteroids are metabolites of steroid hormones e.g. progesterone
bind at same time as GABA
endorphins ?
Endorphins were discovered in 1975 and are naturally occurring small proteins or peptides, including:
endorphin, enkephalin, dynorphin
opioid receptors ? where, types, how they work
are widely distributed in the CNS but concentrated in nociceptive areas have at least 3 main types Include mu (µ), kappa (), sigma ()
Can prevent voltage-gated calcium channels opening or increase opening of potassium channels, both hyperpolarise the cell.
Also decrease cAMP production
where opiates act as drugs
Spinal - block pain signal (analgaesia)
Periaqueductal grey - regulates sensation of “pain”
Amygdala - regulates emotional component
Frontal cortex - cognitive aspects
Brain stem (medulla) - depress respiration and cough e.g. codeine reflex (may induce vomiting)
Analgesia:
- reduces perception of and emotional response to pain
Intestinal disorders:
- reduces diarrhoea; decreases dehydration
Antitussive:
- cough suppressant (codeine)
issues with therapeutic use of opiates
Serious side effects:
Respiratory depression
Sedation
Constipation
Tolerance develops – reduced clinical effect
Dependence develops – leads to withdrawal symptoms
Relieve dull visceral pain better than sharp pain