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Psychofarmology - College 3 - Coggle Diagram
Psychofarmology - College 3
Constitutive activity =
general state, neutral, not turned off, but minimal activity.
Neurotransmitter transporters
A lot of medication we use, attach to either a transporter or an enzyme.
An action needs to be terminated after some point. After the neuron fired.
(ATPase provides energy.)
30% of the medication we use, works through either
stimulating or blocking
a 12-transmembrane (12 parts going through the membrane) receptors.
30% works on effecting the functioning of the ion channels
20% 4-transmembrane (ligand-gated)
10% 6-transmembrane (voltage-sensitive)
30% works on the 7-transmembrane receptors (G-protein-linked)
Other medication works through
inhibition
of emzymes (10%)
Plasma membrane transporters
= they take the neurotransmitter out of the synaptic cleft so they can use it again in the
presynaptic
neuron. From synaps intro presynaptic neuron. Two main classes:
SLC6
(SERT, NET, DAT, GAT, GlyT)
SLC1
(only glutamate)
Vesicular transporters (intracellular):
Second transporter.
In neuron into the vesicles for storage and safety.
Already in neuron.
Three classes:
SLC18
(VMAT, VAChT)
SLC32
(VIAAT)
SLC17
(VGluT1-3)
Competitive inhibition
= when there are two substances. for example, if you take speed/aphetamine. This will replace dopamine in DAT and eventually there will be more dopamine in the synaptic cleft. -> longer effect.
& vesicles are filling themselves with speed and are excreting the dopamine out of the neuron also in the synaptic cleft. -> being euphoric, happy, energetic for a longer time.
Ion channels
= are mostly pentamers (5 different parts).
Calcium
Chloride
Sodium
Kalium/Potassium
Agonist
= ON
Fully active.
The activity in the cell.
Maximum signal transduction.
Partial agonist
=
Partially on.
Netto agonist
= increases low activity
Netto antagonist
= decreases high activity
(Silent) Antagonist
= Blocks
(partial) agonists, inhibits activity.
Goes back to constitutive activity.
Inverse agonist:
Total inactivation. Doing nothing at al
Allosteric modulation
= changing something that is happening. changing the activity of the receptors. Is a secondary receptor (primary receptor is the neurotransmitter).
Only work when neurotransmitter is present. Two types of modulators:
PAM
=
Positive allosteric modulation. Positive, because stimulating effect on ion channel.
NAM
=
Negative allosteric modulation. Negative, because inhibiting effect on ion channel.
Enzymes
=
Creates products
Destroys products
ATPase (energy)
Kinase/Phosphatase
RNA polymerase
Irreversible inhibitor
= suicide. Substrate cannot bind anymore. Cannot be reversed. Death of enzyme.
Substrate binds to enzyme
Enzyme converts substrate to product
Product is released from enzyme
Reversible inhibitor
= substrate. Bound with ropes. Can be reversed.