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32 Cards in this Set

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  • Back
Where is serotonin produced?
1. 95% by enterochromaffin cells in GI tract

2. 5% in CNS
Serotonin in the CNS is highly relevant to what?
Mood stabilization and neurological activity
What is interesting about the effects of serotonic?
It only MODULATES the responses caused by other NT

No direct effects itself
What are 4 neurological functions associated with serotonin?
Mood (depression and axiety)

Sleep

Learning and memory

Behavior inhibition and impulsivity
Serotonin is synthesized from what compound?
Tryptophan
The 5-HT N-acetyl-transferase in the pineal gland in responsible for the conversion of serotonin to what?
Melatonin
What enzyme is the rate limiting step in the serotonin synthetic pathway?
Tryptophan hydroxylase (TPH)
What 2 genes regulate synthesis of TpH?
1. Tph1 in periphery

2. Tph2 in the brain
What happens to serotonin production in response to stress?
It increases
What is the problem with the 5-HTP (cmpd before 5-HT) as a supplement?
Skips rate limiting step BUT has tough time getting through BBB and much gets broken down in periphery
Where is serotonin stored?
In nerve endings, in vesicles where they are protected from degredation
Vesicle membranes contain what uptake transport mechanism?
VMAT - same as that for catecholamines and dopamine
Exocytotic release of serotonin is dependent on what ion?
Calcium
Exocytotic release of serotonin is regulated in part by what?
Autoreceptors
How many serotonin receptors are there?
7 (5-HT 1-7)
The majorty of 5-HT receptors are what type of receptors?
GCPR
What is the only 5-HT receptor which is NOT a GPCR?
5HT3 (ion channel)
What is the significance of the 5HT3 channel?
Mediates vomiting (makes you vomit)
What are autoreceptors?
Pre-synaptic receptors that regulate release
What are the 3 mechanisms of termination of the actions of serotonin?
1. Reuptake into nerve terminals - SERT transporter

2. Metabolic transformation / catabolism

3. Diffusion and uptake at extraneuronal sites
What inactivates both circulation and intraneuronal amines?
Monoamine oxidase (MOA)
What MOA isozymes degrades serotonin?
MAO A
What is the other enzyme that degrades 5-HT?
Aldehyde Dehydrogenase
What is the product of both degredative enzymes?
5-hydroxyindoleactic adic

5-HIAA
What is the role of odansetron?
Receptor antagonist: used as antivomiting medication

Used in chemo
Busprione is used in the treatment of what?

Its MOA?
Partial 5-HTR agonist

Used in anxiety treatment
What MOA is most important in 5-HT pharmacologic manipulation?
Reuptake inhibitor
What type of drugs affecting serotonin are used to treat depression?
SSRI - inhibits reuptake via blocking SERT

MAOI - reduce catabolism of 5-HT
Sumitriptan treats what and has what MOA?
5-Ht receptor agonist that treats migraine
Hallucinogenic drugs target what?
5-HT receptor agonist
Amphetamines and MDMA target what?
Induce vesicular release of serotonin, reverses direction of SERT
Are most drugs in the CNS very specific?
NO, most have overlap