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SEROTONINOPTOM 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)AzapironesSumatriptanCisapride
5-HT ANTAGONISTS.
CYPROHEPTADINE
-CLOZAPINERISPERIDONEONDANSETRON