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Effects of Tianeptine on The Activity of Glutamate Transporter EAAT3 Expressed in Xenopus Oocytes

생물치료정신의학 2020년 26권 3호 p.243 ~ 250
구본욱, 나효석, 유정희, 최정석, 도상환, Zuo Zhiyi,
소속 상세정보
구본욱 ( Koo Bon-Wook ) - Seoul National University Bundang Hospital Department of Anesthesiology and Pain Medicine
나효석 ( Na Hyo-Seok ) - Seoul National University Bundang Hospital Department of Anesthesiology and Pain Medicine
유정희 ( Ryu Jung-Hee ) - Seoul National University Bundang Hospital Department of Anesthesiology and Pain Medicine
최정석 ( Choi Jung-Seok ) - SMG-SNU Boramae Medical Center Department of Psychiatry
도상환 ( Do Sang-Hwan ) - Seoul National University Bundang Hospital Department of Anesthesiology and Pain Medicine
 ( Zuo Zhiyi ) - University of Virginia Health System Department of Anesthesiology

Abstract


Objectives : Tianeptine is an antidepressant that has drawn attention recently. Unlike traditional monoaminergic antidepressants, tianeptine is known to affect glutamate neurotransmission like ketamine. However, there has been paucity of studies investigating the role of tianeptine on glutamate transporters, especially excitatory amino acid transporter type 3 (EAAT3).

Methods : After expression of EAAT3 by intracellular injection of EAAT3 mRNA, we investigated the effect of tianeptine on the activity of EAAT3, by measuring membrane current in response to L-glutamate administration using Xenopus oocyte expression system and two-electrode voltage clamps.

Results : Tianeptine (1mM for 72h) significantly reduced Vmax (6.9±0.6 vs. 4.8±0.3mC, n=14-22, p<0.05) without changing Km (27.0±7.6 vs. 23.3±4.9mM, n=14-22, p=0.72).

Conclusion : When tianeptine was exposed for 72h, it decreased the activity of EAAT3 in a concentration-dependent manner (1-100mM). Our results suggest that tianeptine decreases EAAT3 activity by reducing the available number or turnover rate of EAAT3.

키워드

Excitatory amino acid transporter 3; Depression; Glutamate; Tianeptine; Xenopus oocyte

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