Serotonin Receptors Flashcards
5-HT 1A locations? (3)
- Cortex, hypothalamus
- Raphe nuclei
5-HT 1A effects on cortex, hypothalamus, and raphe nuclei?
- Mood, cognitive function, neuroendocrine function
- Raphe: inhibits 5-HT release
5-HT 1D locations? (2)
- Cerebral vascular smooth m.
- Nerve terminal
5-HT 1D effects on cerebral vascular smooth m. and nerve terminals?
- Vasoconstriction
- Inhibits NT release from nerve terminals (e.g. nociceptive and inflammatory mediators in migraines)
5-HT 2A/2C locations? (2)
- Striatum
- Frontal cortex
5-HT 2A/2C effects on the striatum and frontal cortex?
Hallucinations via inhibiting DA release
5-HT 3 locations? (3)
- Enteric chromaffin cells
- Area postrema
- Emetic center
5-HT 3 effects on the enteric chromaffin cells, area postrema, and emetic center?
Gut motility, N/V
5-HT 4 location? (1)
Myenteric plexus (ENS)
5-HT 4 effect on myenteric plexus?
Gut motility
5-HT transporter location?
5-HT nerve terminals
5-HT transporter effect on 5-HT nerve terminals?
Removal of 5-HT from synapse
What 5-HT receptor does buspirone effect, + specific type of agonism/antagonism?
Associated clinical disorders?
5-HT 1A partial agonist
- Anxiety, depression
What 5-HT receptor does sumatriptan effect, + specific type of agonism/antagonism?
Associated clinical disorder?
5-HT 1D agonist
- Migraine
What 5-HT receptor does trazadone effect, + specific type of agonism/antagonism?
Associated clinical disorders?
What medication is it contraindicated with?
SARI; 5-HT 2A/2C antagonist + SSRI (5-HT xporter inhibitor)
- Depression, schizophrenia (contraindicated w/MAO inhibitors)
What 5-HT receptor does ondansetron effect, + specific type of agonism/antagonism?
Associated clinical disorder?
5-HT 3 antagonist
- Chemo-induced emesis
What 5-HT receptor does mosapride (UK) effect, + specific type of agonism/antagonism?
Associated clinical disorders?
1 serious side-effect? (think)
5-HT 4 agonist
- GI disorders
- SE: arrhythmia (lengthens QT)
What 5-HT receptor does fluoxetine/sertraline effect, + specific type of agonism/antagonism?
Associated clinical disorders?
W/what medication are they contraindicated?
5-HT transporter inhibitor
- Depression, panic disorder, OCD, PTSD, social phobia
Contraindicated w/MAO inhibitors (Serotonin syndrome)
What 5-HT receptor does risperidone effect, + specific type of agonism/antagonism?
Associated clinical disorders?
*Which 2 DA pw’s does it affect and how?
2nd gen anti-psychotic: 5-HT 2A + D 2/3 antagonist
- Schizophrenia w/psychosis
- Suppresses DA release in mesolimbic pw (reduce psychosis via D 2/3), increases DA release in mesocortical pw (reduce hallucinations via 5-HT 2A)
What receptor does L-DOPA effect, + specific type of agonism/antagonism?
Associated clinical disorder?
Serious side effects?
D 1/2 receptor agonist (increases DA in nigrostriatal pw)
- PD
SE: Arrhythmia, dyskinesia
What enzyme does carbidopa effect? Positively or negatively?
Associated clinical disorder?
Targets AADC (makes DA from L-DOPA) in peripheral tissues - PD
What receptor does bromocriptine effect, + specific type of agonism/antagonism?
Associated clinical disorder?
D 2/3 receptor agonist
- PD
What receptor does selegiline effect, + specific type of agonism/antagonism?
Associated clinical disorder?
Serious side effects?
Contraindicated w/what medication?
MAO-B selective antagonist
- PD (early)
SE: Hypotension, hypertensive crisis
- Sympathomimetics
What enzyme does tolcapone effect? Positively or negatively?
Associated clinical disorder?
Contraindicated w/what dz?
Inhibits COMT
- PD (advanced)
Liver failure
What receptor does haloperidol effect, + specific type of agonism/antagonism?
Associated clinical disorder?
D2 antagonist
- Psychosis
What receptor does metaclopramide effect, + specific type of agonism/antagonism?
Associated clinical disorder?
Major side effects?
D2 antagonist + 5-HT 4 agonist properties
- Nausea
SE: akathisia, focal dystonia
