Penghambat penyerapan kembali asam amino eksitatori (Bahasa Inggris: excitatory amino acid reuptake inhibitor, disingkat EAARI) adalah jenis obat yang menghambat penyerapan kembali neurotransmiter eksitatori aspartat dan glutamat dengan memblokir satu atau lebih transporter asam amino eksitatori (EAAT).
Contoh EAARI termasuk asam dihidrokainat (DHK) dan WAY-213,613; penghambat selektif EAAT2 (GLT-1),[1][2] dan L-trans-2,4-PDC; penghambat non-selektif kelima EAAT.[3] Amfetamin adalah penghambat penyerapan kembali nonkompetitif selektif dari EAAT3 presinaptik (melalui endositosis transporter) pada neuron dopamin.[4][5][6] L-Teanina dilaporkan menghambat penyerapan kembali secara kompetitif pada EAAT1 (GLAST) dan EAAT2 (GLT-1).[7]
Lihat juga
sunting- Penghambat penyerapan kembali
- Glutamatergik
- Penghambat penyerapan kembali GABA
- Penghambat penyerapan kembali glisina
- Agonis reseptor asam amino eksitatori
- Antagonis reseptor asam amino eksitatori
Referensi
sunting- ^ J. Storm-Mathisen; O.P. Ottersen (3 November 2000). Glutamate. Elsevier. hlm. 49. ISBN 978-0-08-053257-8.
- ^ Dunlop J, McIlvain HB, Carrick TA, et al. (October 2005). "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. doi:10.1124/mol.105.012005. PMID 16014807. S2CID 24207924.
- ^ Susan Napier; Matilda Bingham (5 May 2009). Transporters as Targets for Drugs. Springer Science & Business Media. hlm. 200. ISBN 978-3-540-87912-1.
- ^ "SLC1A1 solute carrier family 1 (neuronal/epithelial high affinity glutamate transporter, system Xag), member 1 [ Homo sapiens (human) ]". NCBI Gene. National Center for Biotechnology Information. Diakses tanggal 11 November 2014.
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.
- ^ Underhill SM, Wheeler DS, Li M, Watts SD, Ingram SL, Amara SG (July 2014). "Amphetamine modulates excitatory neurotransmission through endocytosis of the glutamate transporter EAAT3 in dopamine neurons". Neuron. 83 (2): 404–16. doi:10.1016/j.neuron.2014.05.043. PMC 4159050. PMID 25033183.
- ^ Revel FG, Moreau JL, Gainetdinov RR, Bradaia A, Sotnikova TD, Mory R, Durkin S, Zbinden KG, Norcross R, Meyer CA, Metzler V, Chaboz S, Ozmen L, Trube G, Pouzet B, Bettler B, Caron MG, Wettstein JG, Hoener MC (May 2011). "TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity". Proc. Natl. Acad. Sci. U.S.A. 108 (20): 8485–8490. Bibcode:2011PNAS..108.8485R. doi:10.1073/pnas.1103029108. PMC 3101002. PMID 21525407.
- ^ Sugiyama T, Sadzuka Y, Tanaka K, Sonobe T (2001). "Inhibition of glutamate transporter by theanine enhances the therapeutic efficacy of doxorubicin". Toxicol. Lett. 121 (2): 89–96. 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.
Pranala luar
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