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Mechanism of Paroxetine (Paxil) Inhibition of the Serotonin Transporter.

Sci Rep. 2016; 
DavisBruce A,NagarajanAnu,ForrestLucy R,SinghSatind
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Mutant Libraries ggSERT and associated mutants were synthesized by GenScript (Piscaway, NJ) and subcloned into pcNoTag. Get A Quote

摘要

The serotonin transporter (SERT) is an integral membrane protein that exploits preexisting sodium-, chloride-, and potassium ion gradients to catalyze the thermodynamically unfavorable movement of synaptic serotonin into the presynaptic neuron. SERT has garnered significant clinical attention partly because it is the target of multiple psychoactive agents, including the antidepressant paroxetine (Paxil), the most potent selective serotonin reuptake inhibitor known. However, the binding site and orientation of paroxetine in SERT remain controversial. To provide molecular insight, we constructed SERT homology models based on the Drosophila melanogaster dopamine transporter and docked paroxetine to the... More

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