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Int. J. Mol. Sci. 2012, 13(3), 2578-2589; doi:10.3390/ijms13032578

Inhibitory Action of Antidepressants on Mouse Betaine/GABA Transporter (BGT1) Heterologously Expressed in Cell Cultures

1 Department of Dental Pharmacology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama 700-8525, Japan 2 RI Research Center, Okayama University Dental School, Okayama 700-8525, Japan 3 Laboratory of Physiology and Anatomy, College of Pharmacy, Nihon University,Funabashi 274-8555, Japan 4 Department of Dental Pharmacology, Hiroshima University Graduate School of Biomedical Sciences, Hiroshima 734-8553, Japan
* Author to whom correspondence should be addressed.
Received: 29 December 2011 / Revised: 28 January 2012 / Accepted: 17 February 2012 / Published: 24 February 2012
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Betaine/γ-aminobutyric acid (GABA) transporter (BGT1, SLC6A12) is a member of the Na+- and Cl-dependent neurotransmitter transporter gene family with a homology to the GABA transporters (GATs), GAT1 (SLC6A1), GAT2 (SLC6A13) and GAT3 (SLC6A11) (HUGO nomenclature). Since antidepressants have been reported to inhibit GABA uptake, we examined those effects on mouse BGT1 (mBGT1) in comparison with other mouse GAT (mGAT) subtypes in the heterologously expressed cell cultures. All antidepressants tested here inhibited the [3H]GABA uptake through mBGT1 and mGATs in a rank order of potency with mBGT1 > mGAT1-3. Kinetic analyses for maprotilline, mianserine and trimipramine revealed that they inhibited mBGT1 and mGAT1 noncompetitively, except that mianserine competitively inhibited mBGT1. These results provided a clue to investigate the structure-function relationship of mBGT1 using antidepressants as a tool, leading to the identification of potential candidates for selective and specific inhibitors of mBGT1.
Keywords: betaine; GABA; transporter; antidepressant; uptake inhibitor betaine; GABA; transporter; antidepressant; uptake inhibitor
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Gerile; Sogawa, C.; Ohyama, K.; Masuko, T.; Kusama, T.; Morita, K.; Sogawa, N.; Kitayama, S. Inhibitory Action of Antidepressants on Mouse Betaine/GABA Transporter (BGT1) Heterologously Expressed in Cell Cultures. Int. J. Mol. Sci. 2012, 13, 2578-2589.

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