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Ligand interaction with the purified serotonin transporter in solution and at the air/water interface
[摘要]

The purified serotonin transporter (SERT) was spread at the air/water interface and the effects both of its surface density and of the temperature on its interfacial behavior were studied. The recorded isotherms evidenced the existence of a stable monolayer undergoing a lengthy rearrangement. SERT/ligand interactions appeared to be dependent on the nature of the studied molecules. Whereas an unrelated drug (chlorcyclizine) did not bind to the spread SERT, it interacted with its specific ligands. Compared to heterocyclic drugs, for which binding appeared to be concentration-dependent, a ‘two-site’ mechanism was evidenced for pinoline and imipramine.

[发布日期]  [发布机构] 
[效力级别]  [学科分类] 生物化学/生物物理
[关键词] Serotonin;Transporter;Surface pressure;Protein monolayer;Serotonin transporter–drug interaction;5-HT;5-hydroxytryptamine (serotonin);SERT;serotonin transporter;RTI (cocaine congener);3β-(4-iodophenylpropene-2β-carboxylic acid methyl ester);MDMA;3;4-methylene dioxymethamphetamine (ecstasy) [时效性] 
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