Chemistry:Excitatory amino acid reuptake inhibitor

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An excitatory amino acid reuptake inhibitor (EAARI) is a type of drug which inhibits the reuptake of the excitatory neurotransmitters glutamate and aspartate by blocking one or more of the excitatory amino acid transporters (EAATs). Examples of EAARIs include dihydrokainic acid (DHK) and WAY-213,613, selective blockers of EAAT2 (GLT-1),[1][2] and L-trans-2,4-PDC, a non-selective blocker of all five EAATs.[3] Amphetamine is a selective noncompetitive reuptake inhibitor of presynaptic EAAT3 (via transporter endocytosis) in dopamine neurons.[4][5][6] L-Theanine is reported to competitively inhibit reuptake at EAAT1 (GLAST) and EAAT2 (GLT-1).[7]

See also

References

  1. ↑ J. Storm-Mathisen; O.P. Ottersen (3 November 2000). Glutamate. Elsevier. p. 49. ISBN 978-0-08-053257-8. https://books.google.com/books?id=hlymxydXZZAC&pg=PA49. 
  2. ↑ "Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2". Mol. Pharmacol. 68 (4): 974–82. October 2005. doi:10.1124/mol.105.012005. PMID 16014807. 
  3. ↑ Susan Napier; Matilda Bingham (5 May 2009). Transporters as Targets for Drugs. Springer Science & Business Media. p. 200. ISBN 978-3-540-87912-1. https://books.google.com/books?id=u5nVEyVchwUC&pg=PA200. 
  4. ↑ "SLC1A1 solute carrier family 1 (neuronal/epithelial high affinity glutamate transporter, system Xag), member 1 [ Homo sapiens (human) "]. National Center for Biotechnology Information. https://www.ncbi.nlm.nih.gov/gene/6505. "Amphetamine modulates excitatory neurotransmission through endocytosis of the glutamate transporter EAAT3 in dopamine neurons. ... internalization of EAAT3 triggered by amphetamine increases glutamatergic signaling and thus contributes to the effects of amphetamine on neurotransmission." 
  5. ↑ "Amphetamine modulates excitatory neurotransmission through endocytosis of the glutamate transporter EAAT3 in dopamine neurons". Neuron 83 (2): 404–16. July 2014. doi:10.1016/j.neuron.2014.05.043. PMID 25033183. 
  6. ↑ "TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity". Proc. Natl. Acad. Sci. U.S.A. 108 (20): 8485–8490. May 2011. doi:10.1073/pnas.1103029108. PMID 21525407. Bibcode: 2011PNAS..108.8485R. 
  7. ↑ "Inhibition of glutamate transporter by theanine enhances the therapeutic efficacy of doxorubicin". Toxicol. Lett. 121 (2): 89–96. 2001. doi:10.1016/s0378-4274(01)00317-4. PMID 11325559. "In addition, RT-PCR and Western blot analysis revealed the expression of GLAST and GLT-1, astrocytic high-affinity glutamate transporters, in M5076 cells. Thus, theanine was shown to competitively inhibit the glutamate uptake by acting on these glutamate transporters.". 

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