Stereoselective inhibition of serotonin transporters by antimalarial compounds
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- 作者：Matthew L. Beckmana ; beckmanm@augsburg.edu" class="auth_mail ; Akula Bala Pramodb ; Danielle Perleyb ; L. Keith Henryb ; keith.henry@med.und.edu" class="auth_mail
- 关键词：5-HT ; serotonin ; dSERT ; Drosophila serotonin transporter ; hSERT ; human serotonin transporter ; SERT ; serotonin transporter ; SSRI ; selective serotonin reuptake inhibitor ; TCA ; tricyclic antidepressant ; TEVC ; two-electrode voltage clamp
- 刊名：Neurochemistry International
- 出版年：July 2014
- 年：2014
- 卷：73
- 期：Complete
- 页码：98-106
- 全文大小：1510 K
文摘
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A number of antimalarials inhibit serotonin transporter (SERT) function.
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Cinchona alkaloids interact with SERT in a stereospecific manner.
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Cinchona alkaloid enantiomers show distinct preference for the S1 or S2 sites.
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Antimalarials may be lead compounds to understand allosteric modulation of SERT.