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32 Cards in this Set
- Front
- Back
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Where is serotonin produced?
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1. 95% by enterochromaffin cells in GI tract
2. 5% in CNS |
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Serotonin in the CNS is highly relevant to what?
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Mood stabilization and neurological activity
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What is interesting about the effects of serotonic?
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It only MODULATES the responses caused by other NT
No direct effects itself |
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What are 4 neurological functions associated with serotonin?
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Mood (depression and axiety)
Sleep Learning and memory Behavior inhibition and impulsivity |
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Serotonin is synthesized from what compound?
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Tryptophan
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The 5-HT N-acetyl-transferase in the pineal gland in responsible for the conversion of serotonin to what?
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Melatonin
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What enzyme is the rate limiting step in the serotonin synthetic pathway?
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Tryptophan hydroxylase (TPH)
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What 2 genes regulate synthesis of TpH?
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1. Tph1 in periphery
2. Tph2 in the brain |
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What happens to serotonin production in response to stress?
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It increases
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What is the problem with the 5-HTP (cmpd before 5-HT) as a supplement?
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Skips rate limiting step BUT has tough time getting through BBB and much gets broken down in periphery
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Where is serotonin stored?
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In nerve endings, in vesicles where they are protected from degredation
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Vesicle membranes contain what uptake transport mechanism?
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VMAT - same as that for catecholamines and dopamine
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Exocytotic release of serotonin is dependent on what ion?
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Calcium
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Exocytotic release of serotonin is regulated in part by what?
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Autoreceptors
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How many serotonin receptors are there?
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7 (5-HT 1-7)
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The majorty of 5-HT receptors are what type of receptors?
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GCPR
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What is the only 5-HT receptor which is NOT a GPCR?
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5HT3 (ion channel)
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What is the significance of the 5HT3 channel?
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Mediates vomiting (makes you vomit)
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What are autoreceptors?
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Pre-synaptic receptors that regulate release
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What are the 3 mechanisms of termination of the actions of serotonin?
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1. Reuptake into nerve terminals - SERT transporter
2. Metabolic transformation / catabolism 3. Diffusion and uptake at extraneuronal sites |
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What inactivates both circulation and intraneuronal amines?
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Monoamine oxidase (MOA)
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What MOA isozymes degrades serotonin?
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MAO A
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What is the other enzyme that degrades 5-HT?
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Aldehyde Dehydrogenase
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What is the product of both degredative enzymes?
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5-hydroxyindoleactic adic
5-HIAA |
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What is the role of odansetron?
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Receptor antagonist: used as antivomiting medication
Used in chemo |
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Busprione is used in the treatment of what?
Its MOA? |
Partial 5-HTR agonist
Used in anxiety treatment |
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What MOA is most important in 5-HT pharmacologic manipulation?
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Reuptake inhibitor
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What type of drugs affecting serotonin are used to treat depression?
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SSRI - inhibits reuptake via blocking SERT
MAOI - reduce catabolism of 5-HT |
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Sumitriptan treats what and has what MOA?
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5-Ht receptor agonist that treats migraine
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Hallucinogenic drugs target what?
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5-HT receptor agonist
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Amphetamines and MDMA target what?
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Induce vesicular release of serotonin, reverses direction of SERT
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Are most drugs in the CNS very specific?
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NO, most have overlap
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