The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors

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• 作者：Akash Pandhare^a ; ^b ; ^{akash.pandhare@ttuhsc.edu} ; Aneesh Satya Pappu^a ; ^e ; ¹ ; ^{apappu@standford.edu} ; Henrik Wilms^c ; ^{henrik.wilms@ttuhsc.edu} ; Michael Paul Blanton^b ; ^d ; ^{michael.blanton@ttuhsc.edu} ; Michaela Jansen^a ; ^b ; ^{michaela.jansen@ttuhsc.edu}
• 关键词：Antidepressant ; Bupropion ; Hydroxybupropion ; 5-HT3A receptors ; Pentameric ligand-gated ion channels
• 刊名：Neuropharmacology
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：113
• 期：part_PA
• 页码：89-99
• 全文大小：1233 K
• 卷排序：113

文摘

Bupropion non-competitively blocked function of 5-HT3ARs in X. laevis oocytes. Bupropion inhibition at these receptors was non-use-dependent. The metabolite hydroxybupropion also inhibited function of 5-HT3ARs in oocytes. Our study establishes the 5-HT3AR as a hitherto unidentified molecular target of bupropion. The study further provides a novel pharmacological basis for bupropion's antidepressant effect.