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5-HT NEUROTRANSMISSION
MR.BESTHA CHAKRAPANI M.pharm
Associate Professor
Department of Pharmacology
Balaji College Of Pharmacy
Ananthapuramu
Serotonin or 5-hydroxytryptamine (5-HT) is a
monoamine neurotransmitter, and is popularly
thought to be a contributor to feelings of well-being
and happiness.
 Biochemically, the indoleamine molecule is derived
from the amino acid tryptophan.
Serotonin is primarily found in the enteric nervous
system located in the gastrointestinal tract (GI tract).
However, it is also produced in the central nervous
system (CNS), specifically in the Raphe nuclei
located in the brainstem.
Additionally, serotonin is stored in blood platelets
and is released during agitation and
vasoconstriction, where it then acts as an agonist to
other platelets.
Approximately 90% of the human body's total
serotonin is located in the enterochromaffin cells in
the GI tract, where it is used to regulate intestinal
movements.
The serotonin is secreted luminally and basolaterally
which leads to increased serotonin uptake by
circulating platelets and activation after stimulation,
which gives increased stimulation of myenteric
neurons and gastrointestinal motility.
The remainder is synthesized in serotonergic neurons of
the CNS, where it has various functions.
 These include the regulation of mood, appetite, and
sleep.
 Serotonin also has some cognitive functions, including
memory and learning.
 Modulation of serotonin at synapses is thought to be a
major action of several classes of pharmacological
antidepressants.
serotonin secreted from the enterochromaffin cells eventually
finds its way out of tissues into the blood. There, it is actively
taken up by blood platelets, which store it.
 When the platelets bind to a clot, they release serotonin,
where it can serve as a vasoconstrictor or a vasodilator while
regulating hemostasis and blood clotting.
In high concentrations, serotonin acts as a vasoconstrictor by
contracting endothelial smooth muscle directly or by
potentiating the effects of other vasoconstrictors (e.g.
angiotensin II, norepinephrine).
The vasoconstrictive property is mostly seen in pathologic
states affecting the endothelium such as atherosclerosis or
chronic hypertension.
 In physiologic states, vasodilation occurs through
the serotonin mediated release of nitric oxide from
endothelial cells.
 Additionally, it inhibits the release of
norepinephrine from adrenergic nerves.
Serotonin is also a growth factor for some types of
cells, which may give it a role in wound healing.
There are various serotonin receptors.
Serotonin is metabolized mainly to 5-HIAA, chiefly
by the liver.
Metabolism involves first oxidation by monoamine
oxidase to the corresponding aldehyde.
 This is followed by oxidation by aldehyde
dehydrogenase to 5-HIAA, the indole acetic acid
derivative. The latter is then excreted by the
kidneys.
Aside from mammals it is found in all bilateral
animals including worms and insects, as well as in
fungi and plants.
Serotonin's presence in insect venoms and plant
spines serves to cause pain, which is a side-effect of
serotonin injection.
 Serotonin is produced by pathogenic amoebae, and
its effect in the human gut is diarrhea.
Its widespread presence in many seeds and fruits
may serve to stimulate the digestive tract into
expelling the seeds.
Serotonin is a neurotransmitter and is found in all
bilateral animals including insects. Serotonin is also
present in plants (phytoserotonin).
Receptors
The 5-HT receptors, the receptors for serotonin, are
located on the cell membrane of nerve cells and
other cell types in animals, and mediate the effects
of serotonin as the endogenous ligand and of a broad
range of pharmaceutical and hallucinogenic drugs.
 Except for the 5-HT3 receptor, a ligand-gated ion
channel, all other 5-HT receptors are G-protein-
coupled receptors (also called seven-transmembrane,
or heptahelical receptors) that activate an
intracellular second messenger cascade.
Thank
you

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5 ht neurotransmission

  • 1. 5-HT NEUROTRANSMISSION MR.BESTHA CHAKRAPANI M.pharm Associate Professor Department of Pharmacology Balaji College Of Pharmacy Ananthapuramu
  • 2. Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter, and is popularly thought to be a contributor to feelings of well-being and happiness.  Biochemically, the indoleamine molecule is derived from the amino acid tryptophan. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract).
  • 3. However, it is also produced in the central nervous system (CNS), specifically in the Raphe nuclei located in the brainstem. Additionally, serotonin is stored in blood platelets and is released during agitation and vasoconstriction, where it then acts as an agonist to other platelets.
  • 4. Approximately 90% of the human body's total serotonin is located in the enterochromaffin cells in the GI tract, where it is used to regulate intestinal movements. The serotonin is secreted luminally and basolaterally which leads to increased serotonin uptake by circulating platelets and activation after stimulation, which gives increased stimulation of myenteric neurons and gastrointestinal motility.
  • 5. The remainder is synthesized in serotonergic neurons of the CNS, where it has various functions.  These include the regulation of mood, appetite, and sleep.  Serotonin also has some cognitive functions, including memory and learning.  Modulation of serotonin at synapses is thought to be a major action of several classes of pharmacological antidepressants.
  • 6. serotonin secreted from the enterochromaffin cells eventually finds its way out of tissues into the blood. There, it is actively taken up by blood platelets, which store it.  When the platelets bind to a clot, they release serotonin, where it can serve as a vasoconstrictor or a vasodilator while regulating hemostasis and blood clotting. In high concentrations, serotonin acts as a vasoconstrictor by contracting endothelial smooth muscle directly or by potentiating the effects of other vasoconstrictors (e.g. angiotensin II, norepinephrine). The vasoconstrictive property is mostly seen in pathologic states affecting the endothelium such as atherosclerosis or chronic hypertension.
  • 7.  In physiologic states, vasodilation occurs through the serotonin mediated release of nitric oxide from endothelial cells.  Additionally, it inhibits the release of norepinephrine from adrenergic nerves. Serotonin is also a growth factor for some types of cells, which may give it a role in wound healing. There are various serotonin receptors.
  • 8. Serotonin is metabolized mainly to 5-HIAA, chiefly by the liver. Metabolism involves first oxidation by monoamine oxidase to the corresponding aldehyde.  This is followed by oxidation by aldehyde dehydrogenase to 5-HIAA, the indole acetic acid derivative. The latter is then excreted by the kidneys.
  • 9. Aside from mammals it is found in all bilateral animals including worms and insects, as well as in fungi and plants. Serotonin's presence in insect venoms and plant spines serves to cause pain, which is a side-effect of serotonin injection.  Serotonin is produced by pathogenic amoebae, and its effect in the human gut is diarrhea. Its widespread presence in many seeds and fruits may serve to stimulate the digestive tract into expelling the seeds.
  • 10. Serotonin is a neurotransmitter and is found in all bilateral animals including insects. Serotonin is also present in plants (phytoserotonin).
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  • 17. Receptors The 5-HT receptors, the receptors for serotonin, are located on the cell membrane of nerve cells and other cell types in animals, and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs.  Except for the 5-HT3 receptor, a ligand-gated ion channel, all other 5-HT receptors are G-protein- coupled receptors (also called seven-transmembrane, or heptahelical receptors) that activate an intracellular second messenger cascade.
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