GABA transporter type 3 (GAT3) uses sodium (Na+) electrochemical gradients to mediate uptake of GABA from the synaptic cleft by surrounding glial cells.[5]
Subtype-selective GAT3 inhibitors are known since 2015.[6]
The transporter and its effect on GABA concentrations in the amygdala has been implicated as a key player in the disease of alcoholism. In studies conducted on rat populations, reduction of GAT3 caused rats who formerly preferred sugar to prefer alcohol. Further, studies of deceased alcoholics show a decreased concentration of GAT3 in their brains.[7]
References
- 1 2 3 GRCh38: Ensembl release 89: ENSG00000132164 – Ensembl, May 2017
- 1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000030307 – Ensembl, May 2017
- ↑ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ↑ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ↑ Kandel ER, Schwartz JH, Jessell TM, Siegelbaum SA, Hudspeth AJ (2013). Principles of Neural Science (Fifth ed.). McGraw-Hill Companies. p. 296. ISBN 978-0-07-139011-8.
- ↑ Damgaard M, Al-Khawaja A, Vogensen SB, Jurik A, Sijm M, Lie ME, Bæk MI, Rosenthal E, Jensen AA, Ecker GF, Frølund B, Wellendorph P, Clausen RP (2015). "Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3". ACS Chem Neurosci. 6 (9): 1591–9. doi:10.1021/acschemneuro.5b00150. PMID 26154082.
- ↑ "A Landmark Study on the Origins of Alcoholism". 21 June 2018.
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| Transporter | | GATTooltip GABA transporter | |
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| VIAATTooltip Vesicular inhibitory amino acid transporter | |
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| Enzyme | | GADTooltip Glutamate decarboxylase | |
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| GABA-TTooltip γ-Aminobutyrate aminotransferase | |
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| Other | |
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- See also
- Receptor/signaling modulators
- GABA receptor modulators
- GABAA receptor positive modulators
- Glutamate metabolism/transport modulators
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