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47 Cards in this Set

  • Front
  • Back
serotonin structure
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serotonin history
1. discovered 1948
2. autocoid and NT
3. most diverse physiological substance in body
serotonin functions-periphery
1. smooth muscle contraction
2. gi enterochromaffin cells (control acid production, gastric motility)
**mediator of pain and itching **opposite of HA
serotonin functions- non-neuronal
platelets, CV system, gi cells (90%)
serotonin functions- CNS
memory, pain (migraine), appetite, sleep, mood and emotions
5HT receptor family
6 types/ 13 subtypes: GCPR
1 type/ 2 subtypes: ligand gated ion channel (Na/K)
4 types: distribution and signalling mechanism
MAKE CHART FOR 5HT TYPES
CHART
5HT chemistry
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5HT at physiological pH
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Biosynthesis of 5HT
Trp-5HTP (Trp Hydroxylase)
5HTP-5HT (L-aromatic amino acid decarboxylase)
Trp structure
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5HTP structure
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5HT metabolism
Major= MAO to 5-hydroxyindolacetic acid
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**diagnostic metabolite for migraine sufferers
5HT metabolism (2)
acetylase-o-methylase
DRUGS
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5HT1 AGONISTS
sumatriptan, zomatriptan, naratriptan
5HT1 PARTIAL AGONISTS
buspirone
5HT4 AGONISTS
cisapride
5HT4 PARTIAL AGONISTS
tegaserod
5HT2 ANTAGONISTS
ketanserin
5HT3 ANTAGONISTS
ondansetron, granisetron, alosetron
NON-SELECTIVE 5HT ANTAGONISTS
cyproheptadine
ergot derivatives (LSD, methysergide, ergotamine, bromocriptine)
sumatriptan structure
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zomatriptan structure
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naratriptan structure
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*better CNS penetration
5HT1 receptor agonists
activate in brain--dec. cAMP
changed OH to sulfonamide, inc lip and inc BBB
5HT1 agonists TX
migraines=abort migraine attack
cranial blood vessels pulsate: dilate and contract
(dec cAMP, relax pulsation)
** relieves aura and active headache, may also inhibit inflammation
buspirone structure
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Tx: anxiety, depression, smoking cessation
5HT4 action?
enteric nerve that innervates esophageal smooth muscle==inc cAMP, = contraction
5HT4 rec. ags. tx?
1. gastric hypomotility
(inc peristalsis and gastric emptying)
2. dec. GERD (now use PPI)
3. constipation
tegaserod structure
tx: IBS, constipation
SE's tegaserod
abdominal pain, diarrhea
dec BP (b/c vasodilation)
emotional lability
ketanserin tx
thromboembolic diseases (dec platelet aggregation)
HTN (vasodilation)
5HT3 antags
LIGAND GATED ION CHANNELS
limit GI motility
tx: nausea, vomiting
alosetron tx
IBS
SE: severe constipation
**off market
ketanserin tx
thromboembolic diseases (dec platelet aggregation)
HTN (vasodilation)
5HT3 antags
LIGAND GATED ION CHANNELS
limit GI motility
tx: nausea, vomiting
alosetron tx
IBS
SE: severe constipation
**off market
5HT1 receptor agonists
activate in brain--dec. cAMP
changed OH to sulfonamide, inc lip and inc BBB
5HT1 agonists TX
migraines=abort migraine attack
cranial blood vessels pulsate: dilate and contract
(dec cAMP, relax pulsation)
** relieves aura and active headache, may also inhibit inflammation
buspirone structure
Tx: anxiety, depression, smoking cessation
5HT4 action?
enteric nerve that innervates esophageal smooth muscle==inc cAMP, = contraction
cisapride structure
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tegaserod structure
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ketanserin structure
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ondansetron structure
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cyproheptadine structure
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.tx: pruritis, hypermotility of GI due to GI cancers