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Fluoxetine and all other SSRIs are 5-HT2B Agonists

ssri antidepressant ht2b fluoxetine

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#1 sativa

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Posted 23 April 2016 - 10:20 AM


Fluoxetine and all other SSRIs are 5-HT2B Agonists - Importance for their Therapeutic Effects

Abstract
Fluoxetine and other serotonin-specific re-uptake inhibitors (SSRIs) are generally thought to owe their therapeutic potency to inhibition of the serotonin transporter (SERT). However, research in our laboratory showed that it affects, with relatively high affinity the 5-HT2B receptor in cultured astrocytes; this finding was confirmed by independent observations showing that fluoxetine loses its ability to elicit SSRI-like responses in behavioral assays in mice in which the 5-HT2B receptor was knocked-out genetically or inhibited pharmacologically. All clinically used SSRIs are approximately equipotent towards 5-HT2B receptors and exert their effect on cultured astrocytes at concentrations similar to those used clinically, a substantial difference from their effect on SERT.

www.ncbi.nlm.nih.gov/pmc/articles/PMC4207076/





Also tagged with one or more of these keywords: ssri, antidepressant, ht2b, fluoxetine

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