Neuropharmacology

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The 5 keys areas that drugs interfere with
Syntheses, storage, release, receptors, removal mechanisms
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iNHIBITION of Synthesis of neurotransmitter has a...
very SLOW onset of action
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An example of enhancing synthesis
L-dopa, which is a dopamine precursor to enhance dopamine production in Parkinsons
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An example of vesicle disruption that can lead to leakage of neurotransitter from nerve terminals
Amphetamines lead to leakage of noradrenaine from noradrenergic terminals
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Ways that release of NT can be inhibited
Blockage of VOCC's by w-conotoxin.
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How has w-conotoxin been used experimentally?
as an analgesic
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What are autoreceptors?
Receptors that mediate feedback of neurotransmitters on its own release process.
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What are heteroreceptors?
Receptors that mediate the inhibitory effects of one neurotransmitters on the release process of another
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Examples of autoreceptors
a2-adrenoreceptors
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examples of heteroreceptors
opioid receptors
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What will antagonists at pre-synaptic inhibitory receptors do?
INCREASE the release of neurotransmitter
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What type of receptor is the GABAa receptor?
Ionotropic
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What kind of receptor is the 5HT3 receptor?
Ionotropic
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What kind of receptor is the d1-d5 receptor
metabotropic
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What kind of receptor is the NMDA and AMPA glutamate receptors
ionotropic
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What does pencyclidine do?
Non-competative antagonist that clocks the channel of the NMDA receptor
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What needs to bind to NMDA receptors for them to activate?
glutamate and glycine as co-aginists
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Which receptor does benzodiazapine bind to?
GABAa
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How does three types of binding to BDZ site alter the effects of GABA
agonists - potentiate the effect. Inverse agonists - inhibit the actions of GABA. antagonists - block the effects of BDZ agonists but has no effect on GABA
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An example of a drug for each type
agonist- diazapam. inverse agonists - RO194602. Antagonists - flumazenil
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Two broad mechanisms for neurotransmitter removal
enzymatic destruction, reuptake
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Three nt's that use enzymatic destruction
Ach, Neuropeptides, ATP.
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A drug that prevents noradrenaline uptake
Cocaine
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A drug that prevents 5HT uptake
fluoxetine
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a drug that prevents ACh uptake
Rivastigmine
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Why will ions flow across the membrane?
In order to move the membrane potential towards it's equilibruim potential.
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Examples of channels opened by exitatory drugs
Na, Ca,
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Examples of channels opened by inhibitory drugs
K, Cl
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An example of longer term effects of NT
Action on D1 receptor to increase adenyl cyclase, lead to changes in protien transcription
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Card 2

Front

iNHIBITION of Synthesis of neurotransmitter has a...

Back

very SLOW onset of action

Card 3

Front

An example of enhancing synthesis

Back

Preview of the front of card 3

Card 4

Front

An example of vesicle disruption that can lead to leakage of neurotransitter from nerve terminals

Back

Preview of the front of card 4

Card 5

Front

Ways that release of NT can be inhibited

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