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31 Cards in this Set
- Front
- Back
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This NT is a monoamine primarily found in the GI tract and CNS.
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Serotonin
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Where is most of the body's serotonin found?
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In the GI tract.
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Where is serotonin secreted from?
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Enterochromaffin cells
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When platelets bind to a clot, they disgorge _________, where it serves as a vasoconstrictor and helps regulate hemostasis and blood clotting.
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serotonin
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Does serotonin have a role in wound healing?
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Yes.
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Serotonin is metabolized to ________ by the liver and excreted by the kidneys.
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5-HIAA
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How many serotonin receptor subtypes are there?
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13
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What is serotonin synthesized from?
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L-tryptophan
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What is the rate limiting enzyme of serotonin synthesis?
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Tryptophan hydroxylase
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What two steps are essential in the transformation of tryptophan into serotonin?
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1. Hydroxylation in 5-hydroxytryptophan
2. Decarboxylation of 5-hydroxytryptophan. |
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In the brain, serotonin biosynthesis depends on what?
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The quantity of tryptophan.
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Should the transformation of serotonin into melatonin be considered a degradation pathway?
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No. Melatonin is an active compound.
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What 2 steps are necessary for the transformation of serotonin into melatonin?
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1. Acetylation of the amine group by N-acetyl transferase.
2. Methylation of the OH group by 5-hydroxyindole-O-methyltransferase. |
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The gut contains ___-____% of the total amount of serotonin in the body?
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80-95%
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Serotonin is partly reuptaken by ________ neurons.
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Presynaptic
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Serotonin is released by ____________ serotonergic neurons in the synaptic cleft.
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Presynaptic
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How is serotonin inactivated?
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Oxidative deamination by MAO, oxidation to 5-HIAA, followed by conjugation.
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A drug effective against nausea and vomiting that is typically used to treat motion sickness and side effects of opioid analgesics.
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Antiemetic
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True or False
Serotonin agonist have antiemetic effects. |
False. Serotonin antagonist.
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Altered bodily perceptions, severe headaches, and nausea.
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Migraine
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True or False
The typical migraine is bilateral, pulsating, and can last up to 72 hours. |
False
Unilateral. |
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What is the cause of migraine headaches thought to be?
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Disorder of the serotonergic control system.
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________ are a family of drugs considered to be a mid-line treatment suitable for typical migraines.
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Triptans
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Triptans are ________ ___________.
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Beta-indole ethylamines
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What is the MOA of triptans?
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They bind to serotonin receptors in cranial blood vessels causing constriction and inhibition of proinflammatory neuropeptide release.
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How are triptans metabolized?
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Metabolized to an active primary amine via N-demethylation. Then metabolized via MAO
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A 5-HT antagonist used for the management of severe diarrhea-predominant IBS in women only?
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Alosetron
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A selective 5-HT agonist for IBS, that is used for IBS constipation in women and chronic idiopathic constipation in men and women?
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Tegaserod
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Name a class of serotonin reuptake inhibitors.
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Antidepressants
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Name a serotonin releaser.
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MDMA
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Name 3 serotonin receptor antagonists
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LSD, Psilocybin, DMT
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