PHRM 211 Lecture Notes - Lecture 19: 5-Ht Receptor, Structural Similarity, Headache

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26 Apr 2020
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Now appears to be a ubiquitous neurotransmitter involved in everything. Serotonin was initially thought to do nothing when initially discovered. Structural similarity between serotonin & lsd prompted scientists to speculate that serotonin can be involved in the mechanism of action of lsd"s psychoactive activities. Serotonin is involved many different central & peripheral actions : anxiety, depression, schizophrenia, drug abuse, sleep, dreaming, hallucinogenic activity, headache, cardiovascular disorders, sexual behavior, appetite control. Serotonin is made from its tryptophan precursor and packaged into presynaptic vesicles. When released, serotonin binds to postsynaptic receptors (g-coupled protein receptors, Activation of receptors through depolarization or dissociation of g-coupled proteins = downstream effects. Phenylpiperazine-triazolopyridine antidepressant (indicated for insomnia, alcohol dependence, depression, anxiety) M-chlorophenylpiperazine (metabolite) 5-ht2c agonist & 5-ht2a antagonist. Acts as a serotonin reuptake inhibitor, but is not considered in the class of ssris because it is chemically distinct. Trazodone therapy has been associated with instances of idiosyncratic hepatotoxicity similar to acetaminophen/napqi.

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