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OPTOM FASLU MUHAMMED
5-HYDROXYTRYPTAMINE
( 5-HT, Serotonin)
-90% : localized in intestine
-rest : platelets and brain.
-also found in plants : banana, pear, pineapple, tomato.
STORAGE, SYNTHESIS & DISTRIBUTION
- It is synthesised from amino acid tryptophan.
- degraded primarily by MAO and to a small extent by
dehydrogenase.
- 5-HT is actively taken up by an amine pump serotonin
transporter (SERT), a Na+ dependant carrier, which
operates at the membrane of platelets and serotonergic
nerve endings.
- This is inhibited by selective serotonin reuptake inhibitors
(SSRIs)
SEROTONIN RECEPTORS
- Based on pharmacological criteria :
- musculotropic ( D type)
- neurotropic ( M type)
- 5 HT receptor types : ( 5 HT1, 5 HT2, 5 HT3, 5 HT4 etc..)
 ACTIONS
- CVS :
arteries are constricted (by action on smooth muscle ) as
well as dilated (through EDRF release) by direct action
of 5-HT.
- SMOOTH MUSCLES
Potent stimulator of g.i.t both by direct action as well as
through enteric plexuses.
5HT containing neurons may regulate peristalsis
 GLANDS
- inhibits gastric secretion ( both acid and pepsin)
- Ulcer protective property
- NERVE ENDINGS AND ADRENAL MEDULLA
- Afferent nerve endings are activated – tingling and
pricking sensation, pain.
-
 RESPIRATION
- stimulation of respiration and hyperventilation.
 PLATELETS
- cause change in shape of platelets
- It’s a weak aggregator of platelets- at the site of injury
 CNS
- given i.v, it does not produce central effects because it
poorly crosses blood brain barrier.
- It’s an inhibitory transmitter.
- Direct injection in the brain produces sleepiness, changes
in body temperature, hunger and a variety of behavioral
effects.
5 HT receptor agonists
 D-lysergic acid diethyl amide (LSD)
 Azapirones
 Sumatriptan
 Cisapride
5-HT ANTAGONISTS.
 CYPROHEPTADINE
-CLOZAPINE
RISPERIDONE
ONDANSETRON

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Serotonin

  • 2. 5-HYDROXYTRYPTAMINE ( 5-HT, Serotonin) -90% : localized in intestine -rest : platelets and brain. -also found in plants : banana, pear, pineapple, tomato.
  • 3. STORAGE, SYNTHESIS & DISTRIBUTION - It is synthesised from amino acid tryptophan. - degraded primarily by MAO and to a small extent by dehydrogenase. - 5-HT is actively taken up by an amine pump serotonin transporter (SERT), a Na+ dependant carrier, which operates at the membrane of platelets and serotonergic nerve endings.
  • 4. - This is inhibited by selective serotonin reuptake inhibitors (SSRIs)
  • 5. SEROTONIN RECEPTORS - Based on pharmacological criteria : - musculotropic ( D type) - neurotropic ( M type) - 5 HT receptor types : ( 5 HT1, 5 HT2, 5 HT3, 5 HT4 etc..)
  • 6.  ACTIONS - CVS : arteries are constricted (by action on smooth muscle ) as well as dilated (through EDRF release) by direct action of 5-HT. - SMOOTH MUSCLES Potent stimulator of g.i.t both by direct action as well as through enteric plexuses. 5HT containing neurons may regulate peristalsis
  • 7.  GLANDS - inhibits gastric secretion ( both acid and pepsin) - Ulcer protective property - NERVE ENDINGS AND ADRENAL MEDULLA - Afferent nerve endings are activated – tingling and pricking sensation, pain. -
  • 8.  RESPIRATION - stimulation of respiration and hyperventilation.  PLATELETS - cause change in shape of platelets - It’s a weak aggregator of platelets- at the site of injury
  • 9.  CNS - given i.v, it does not produce central effects because it poorly crosses blood brain barrier. - It’s an inhibitory transmitter. - Direct injection in the brain produces sleepiness, changes in body temperature, hunger and a variety of behavioral effects.
  • 10. 5 HT receptor agonists  D-lysergic acid diethyl amide (LSD)  Azapirones  Sumatriptan  Cisapride