5-ht Flashcards
5-ht 1 receptors where are they used
main in CNS
activation results in neural inhibition and vasoconstriction
important in mood and behaviour, thermoregulation, feeding and sleeping
5-ht in migraines
can cause vasoconstriction in cerebral arteries
5-hiaa found in urine of patcients with migranes
antagonists, sumitriptan
5-ht 1 anatagonists
none in clinical use
methiothepin
methiothepin what does it act on
all the 5-ht1 receptor subtypes
5-ht2 receptors where do they act
CNS
also distributed in periphery
agonist of 5-ht2
LSD
causing hallucinations
LSD is also a
antagonist of the 5-ht2 recpetor in the periphery
action of LSD
inhibits firing of 5-ht neurons
alters perception (sound sight)
have been reported to precipitate attacks in schizophrenia patients
5-ht in gut what does it stimulate
stimulates GI motality both directly and indirectly
directly via 5-ht2 via smooth muscle contraction
indirectly via 5-ht3 and 4 receptors on enteric neurons
what is also stimulated in the gut
fluid secretion and elicit nausea and vomiting by stimulating 5-ht receptors in the stomach
peristalsis mediated by 5-ht release from what
chromaffin cells
by distention of the gut
5-ht in cardiovascular system
action depends on size of vessel, species sympathetic activity
direct and indirect effect
direct (NO release from endothelial cells)
indirect : inhibitory nor release from sympathetic nerve terminals
in the cardiovascular system what does injection of 5-ht do
initial increase in blood pressure
as large vessels contract followed by a fall as the artieriole dilate
5- ht in platelets
5-ht and 5-ht2 on platelet trigger the release of more 5-ht and causes platelets to become sticky
adhesion
platelet plug
5-ht 2 antagonists
methysergide
ketotifen
the effects of methysergide and ketotifen
many antagonists affect other 5-HT receptors as well as a-adrenoceptors and histamine receptors
methysergide - used to treat migranes
5-ht3 receptors where are they found
peripheral nervous system - invoke pain
brain - involved in vomiting reflex
antagonists of 5-ht3
ondansetron
what does ondansetron do
used as anti emetics
controls server vomiting and nausea in chemotherapy
5-ht 4 receptors where are they found
CNS
also regulate GI motility
antagonists of 5-ht4
tegaserod
what does tegaserod do
treats irritable bowel syndrome
how to regulate serotonin
mao inhibitors
selective 5-ht uptake inhibitors
moa inhibitors what does it do
stops 5-hiaa production