Inhibitory Action of Antidepressants on Mouse Betaine/GABA Transporter (BGT1) Heterologously Expressed in Cell Cultures
Abstract
:1. Introduction
2. Results
2.1. Establishment of the GAT-Expressing Cell Lines
2.2. Comparison of the Inhibitory Potency of Antidepressants
2.3. Kinetic Analyses of the Effects of Antidepressants on BGT1
3. Discussion
4. Experimental Section
4.1. Materials
4.2. cDNA Constructs
4.3. Cell Culture and Expression
4.4. Uptake Assay
4.5. Statistical Analysis
5. Conclusions
Supplementary Information
ijms-13-02578-s001.pdfAcknowledgments
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Drugs | IC50 (μM) | ||||
---|---|---|---|---|---|
mBGT1 | mGAT1 | mGAT2 | mGAT3 | rSERT | |
Amitriptyline | 33.0 ± 9.9 * | 100.6 ± 11.7 | 45.8 | 61.5 | 0.14 |
Amoxapine | 78.3 ± 9.5 * | 287.9 ± 80.5 | 134.6 | 195.4 | 1.62 |
Clomipramine | 27.2 ± 6.1 | 93.3 ± 39.8 | 41.8 | 40.2 | 0.05 |
Desipramine | 75.3 ± 6.3 * | 268.4 ± 36.7 | 122.5 | 80.3 | 1.23 |
Doxepine | 59.9 ± 11.2 ** | 222.1 ± 14.7 | 129.2 | 115.5 | 0.58 |
Imipramine | 44.5 ± 2.2 * | 222.5 ± 58.5 | 105.9 | 108.1 | 0.75 |
Maprotilline | 61.3 ± 2.1 ** | 123.5 ± 8.4 | 98.0 | 106.1 | 27.5 |
Mianserine | 57.4 ± 3.9 ** | 221.6 ± 9.9 | 131.1 | 91.0 | 7.63 |
Nortriptyline | 47.0 ± 2.1 * | 135.7 ± 21.9 | 87.1 | 74.1 | 0.63 |
Protriptyline | 43.6 ± 10.2 ** | 166.8 ± 22.1 | 77.2 | 113.0 | 0.91 |
Trimipramine | 21.8 ± 3.8 * | 181.4 ± 72.9 | 85.6 | 64.6 | 5.89 |
Transporter | Drugs | Km (μM) | Vmax (ratio to control #) |
---|---|---|---|
mGAT1 | Control | 13.04 ± 1.87 | 1.00 |
Maprotiline | 9.38 ± 2.44 | 0.48 ± 0.04 * | |
Mianserine | 9.93 ± 2.67 | 0.47 ± 0.04 * | |
Trimipramine | 9.33 ± 2.39 | 0.37 ± 0.05 * | |
mBGT1 | Control | 202.2 ± 34.8 | 1.00 |
Maprotiline | 242.7 ± 56.2 | 0.47 ± 0.06 * | |
Mianserine | 305.2 ± 56.4 * | 0.90 ± 0.03 | |
Trimipramine | 254.9 ± 34.4 | 0.86 ± 0.06 |
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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. https://doi.org/10.3390/ijms13032578
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. International Journal of Molecular Sciences. 2012; 13(3):2578-2589. https://doi.org/10.3390/ijms13032578
Chicago/Turabian StyleGerile, Chiharu Sogawa, Kazumi Ohyama, Takashi Masuko, Tadashi Kusama, Katsuya Morita, Norio Sogawa, and Shigeo Kitayama. 2012. "Inhibitory Action of Antidepressants on Mouse Betaine/GABA Transporter (BGT1) Heterologously Expressed in Cell Cultures" International Journal of Molecular Sciences 13, no. 3: 2578-2589. https://doi.org/10.3390/ijms13032578