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