2016 Fiscal Year Final Research Report
Elucidation of neural GABA transporter function by developing novel subtype-selective inhibitors
| Project/Area Number |
15K14960
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Pharmacology in pharmacy
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| Research Institution | Hokkaido University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
SHUTO Satoshi 北海道大学, 大学院薬学研究院, 教授 (70241346)
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Keywords | 脳・神経 / 薬理学 / 有機化学 / ＧＡＢＡ / トランスポーター / 創薬 |
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| Outline of Final Research Achievements |
Compound B, a candidate of the selective inhibitor for the BGT-1 subtype of the GABA transporters, showed an antidepressant effect in the tail suspension test. This compound showed high binding affinity and agonistic activity on GABAA receptors. It did not bind to GABAB receptors. These results suggested that the antidepressant effect of the compound B is due to the inhibition of BGT-1 or the combined action of BGT-1 inhibition and GABAA receptor activation. In order to obtain a compound which does not act on GABA receptors but inhibits BGT-1 selectively, four compounds were newly synthesized. However, none of them showed BGT-1 inhibitory effect.
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| Free Research Field |
神経薬理学
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