Lecture 14, drugs affecting serotonin Flashcards
why are 5Ht1 receptors inhibitory?
coupled to Gi/Go proteins which inhibit cAMP formation
how does binding to 5-HT1 trigger hyperpolarisation?
activates GiRK
along with 5-HT1A, which other receptor reduces serotonin release upon activation?
5-HT1B
what is the effect of 5-HT1A and 5HT1b receptors on non-serotonergic receptors?
inhibit release of other neurotransmitters
5-Ht1A/b receptor location
post and pre synaptically
which channels are activated upon activation of 5-Ht1a/B receptors on post-synaptic membrane?
GiRk
migranes can be treated with
serotonin receptor agonists
how does sumatriptan exert its effects?
binds to presynaptic 5-HT1 receptors to inhibit proinflammatory peptide and neuropeptide release
binds post-synaptically to trigger vasoconstriction
why is Lasmiditan suitable in treating migraines in those with vascular disease?
doesnt trigger vasoconstriction
which drug targets 5-HT1F receptors
Lasmiditan
migraine involved the activation of which sensory nerves?
trigeminal
activation of 5-Ht3 receptors causes what movement?
inward movement of K, Na and Ca
release of serotonin, CCK, gabba and dopamine is triggered by activation of what kind of serotonin receptor?
presynaptic 5-HT3
where are post synaptic 5-HT3 receptors located?
hippocampus
how does ondansetron prevent drug-induced vomiting
5-HT3 receptor antgagonist
prevents activation vagal afferents in periphery
which central regions does ondanestron prevent the activation of in response to a cytotoxic drug?
area postrema and the nucleus tractus solitatus- vomiting centre not innervated
why do SSRis cause an initial decrease in mood?
serotonin increase in the synaptic cleft activates autoreceptors which decreases serotonin release
SSRIS inhibit
SERT
activation of autoreceptors effect on 5HT
decrease levels
which decreases sensitivity of autoreceptors
decreases amount of 5ht metabolites have been associated with
suicide and aggression
low serotonin revels in those who tried to kill themseleves may be due to an increase in what type of receptor?
a 5-Ht1utoreceptors in the raphe nucleus
Moncrief:
may not be a link between serotonin and depression
5-HT2CR knock out is associated with what affect on appetite?
an increase
Lorcaserin is an agonist for which receptor?
5-HT2C
binding of lorcaserin to 5-HT2C receptors causes what change to weight?
a decrease
why was lorcaserin no longer FDA-approved in 2020?
slightly increases cancer incidence
reuptake inhibitors had what effect on emotional aversion to harm?
increases it
describe the connection between PTSD and serotonin.
increase in 5-HT1A receptors in PTSD group
how did MDMA along with therapy differ from therapy on its own in PTSD treatment?
combined treatments resulted in more: remission, loss of the diagnosis, and responders
which serotonin receptor is implicated in OCD?
5-HT7
variations of SERT in OCD
genetic
epigenetic (methylation)
genetic connotations in OCD involve
gender and age of onset
which serotonin receptor is implicated in Alzheimers treatment?
5-HT4
5-HT4 receptors are involved in which pathway?
non-amyloidogenic
implication of 5-HT4 receptor in alzheimers
activation stimulates ADAM-10 which cleaves APP
which drugs may be beneficial in alzheimers treatment
5-HT4 agonists
selective 5-HT4 agonists bring about what effects?
reduction in plaques
increase in sAPP alpha
decreases inflammation
better cognition
selective 5-HT4 agonists improve function of which brain region?
hippocampus
behavioral functions of serotonin
temperature regulation
sleep and wake cycle
ibs
pain
