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Serotonin/ Agonists
Understanding receptors
15
Pharmacology
Graduate
02/23/2011

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Term
Serotonin
Definition
endogenous
made from tryptophan
neurotransmitter
widely found in nature
Term
GI effect of serotonin
Definition
initiates peristalsis
Term
platelets and serotonin
Definition
Platelets uptake 5-HT and store it in secretory granules. Platelet aggregation triggers 5-HT release and vasoconstriction
Term
Carcinoid tumor and serotonin
Definition
psychotic behaviors may result from tumors of the enterochromaffin cells that excrete high amounts of 5-HT into circulation
Term
5-HT1 receptors
Definition
Five members
expressed by neurons in the CNS
G protein coupled receptors
Inhibit adenylate cyclase
regulate ion channels
inhibit neuronal 5-HT release
Term
5-HT1 agents
Definition
Buspirone
LSD
Sumitriptan
Term
5-HT2 receptors
Definition
G protein coupled
Activate PL-c
Increase intracellular calcium
brain, gut, and platelets
Term
5-HT2 receptor agents
Definition
Methysergide
ketanserin
cyproheptadine
Term
5-HT3 receptors
Definition
ligand gated ion channels
Cause cell depolarization
brain, GI tract, spurs emetic response
Term
5-HT4 receptors
Definition
GProtein coupled
activate adenylate cyclase
CNS and GI tract
mediate secretion and peristalsis
Term
5-HT 1b/1d agonists
Definition
e.g. Sumatriptan
used for acute treatment of migraine, not prophylaxis
contra in patients with CV, brain dz
Raise serotonin levels
SQ dosing to avoid nausea/vomit
Term
serotonin syndrome
Definition
serotonin excess that is fatal
SSRI + 'triptans
cognitive + autonomic dysfunctions
Term
5-HT 2A/2C Antagonists
Definition
e.g. methysergide
used prophylactically for migraines but not a first line tx
long term therapy not good; metabolite is psychidelic, inflammatory fibrosis
Term
5-HT 3 antagonists
Definition
e.g. ondansetron
treat nausea, but not motion sickness
Side effects: constipation
Term
5-HT4 agonists
Definition
e.g. metoclopramide, mosapride
prokinetic, upper GI emptying
treats GERD and IBS
relieves GI dysmotility syndromes
anti-dopaminergic effect
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