MGS-0039
IUPAC ime | |
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(1R,2R,3R,5R,6R)-2-amino-3-(3,4-dihlorobenziloksi)-6-fluorobiciklo[3.1.0]heksan-2,6-dikarbokskilna kiselina | |
Pravni status | |
Pravni status |
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Identifikatori | |
CAS broj | 569686-87-9 Y |
ATC kod | None |
PubChem | CID 9886034 |
ChemSpider | 8061707 |
Hemijski podaci | |
Formula | C15H14Cl2NO5 |
Molarna masa | 378,179 g/mol |
SMILES
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InChI
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MGS-0039 je lek koji se koristi u naučnim istraživanjima. On deluje kao potentan i selektivan antagonist grupe II metabotropnih glutamatnih receptora (mGluR2/3).[1][2] On proizvodi antidepresivne i anksiolitičke efekte u životinjskim studijama,[3][4][5][6] i pokazano je da pojačava otpuštanje dopamina i serotonina u specifičnim oblastima mozga.[7][8] Istraživanja pokazuju da do toga može doći sličnim mehanizmom kao i kod srodnog glutaminergičnog leka ketamina.[9][10]
Reference
- ^ Chaki S, Yoshikawa R, Hirota S, Shimazaki T, Maeda M, Kawashima N, Yoshimizu T, Yasuhara A, Sakagami K, Okuyama S, Nakanishi S, Nakazato A. MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity. Neuropharmacology. 2004 Mar;46(4):457-67. PMID 14975669
- ^ Nakazato A, Sakagami K, Yasuhara A, Ohta H, Yoshikawa R, Itoh M, Nakamura M, Chaki S. Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists. Journal of Medicinal Chemistry. 2004 Aug 26;47(18):4570-87. PMID 15317467
- ^ Shimazaki T, Iijima M, Chaki S. Anxiolytic-like activity of MGS0039, a potent group II metabotropic glutamate receptor antagonist, in a marble-burying behavior test. European Journal of Pharmacology. 2004 Oct 6;501(1-3):121-5. PMID 15464070
- ^ Yasuhara A, Nakamura M, Sakagami K, Shimazaki T, Yoshikawa R, Chaki S, Ohta H, Nakazato A. Prodrugs of 3-(3,4-dichlorobenzyloxy)-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (MGS0039): a potent and orally active group II mGluR antagonist with antidepressant-like potential. Bioorganic and Medicinal Chemistry. 2006 Jun 15;14(12):4193-207. PMID 16487713
- ^ Yoshimizu T, Shimazaki T, Ito A, Chaki S. An mGluR2/3 antagonist, MGS0039, exerts antidepressant and anxiolytic effects in behavioral models in rats. Psychopharmacology (Berlin). 2006 Jul;186(4):587-93. PMID 16612616
- ^ Stachowicz K, Wierońska J, Domin H, Chaki S, Pilc A. Anxiolytic-like activity of MGS0039, a selective group II mGlu receptor antagonist, is serotonin- and GABA-dependent. Pharmacological Reports. 2011;63(4):880-7. PMID 22001975
- ^ Kawashima N, Karasawa J, Shimazaki T, Chaki S, Okuyama S, Yasuhara A, Nakazato A. Neuropharmacological profiles of antagonists of group II metabotropic glutamate receptors. Neuroscience Letters. 2005 Apr 22;378(3):131-4. PMID 15781145
- ^ Karasawa J, Yoshimizu T, Chaki S. A metabotropic glutamate 2/3 receptor antagonist, MGS0039, increases extracellular dopamine levels in the nucleus accumbens shell. Neuroscience Letters. 2006 Jan 30;393(2-3):127-30. PMID 16233956
- ^ Pałucha-Poniewiera A, Wierońska JM, Brański P, Stachowicz K, Chaki S, Pilc A. On the mechanism of the antidepressant-like action of group II mGlu receptor antagonist, MGS0039. Psychopharmacology (Berlin). 2010 Dec;212(4):523-35. PMID 20703449
- ^ Koike H, Iijima M, Chaki S. Involvement of the mammalian target of rapamycin signaling in the antidepressant-like effect of group II metabotropic glutamate receptor antagonists. Neuropharmacology. 2011 Dec;61(8):1419-23. PMID 21903115
Spoljašnje veze
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Grupa I | Agonisti: Neselektivni: ACPD • DHPG • Kuiskualinska kiselina; mGlu1-selektivni: Ro01-6128 • Ro67-4853 • Ro67-7476 • VU-71; mGlu5-selektivni: ADX-47273 • CDPPB • CHPG • DFB • VU-1545 Antagonisti: Neselektivni: MCPG • NPS-2390; mGlu1-selektivni: BAY 36-7620 • CPCCOEt • LY-367,385 • LY-456,236; mGlu5-selektivni: DMeOB • Fenobam • LY-344,545 • MPEP • MTEP • SIB-1757 • SIB-1893 |
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Grupa II | Agonisti: Neselektivni: CBiPES • DCG-IV • Eglumegad • LY-379,268 • LY-404,039 • LY-487,379 • MGS-0028; mGlu2-selektivni: BINA • LY-566,332 Antagonisti: Neselektivni: APICA • EGLU • HYDIA • LY-307,452 • LY-341,495 • MCPG • MGS-0039; mGlu2-selektivni: PCCG-4; mGlu3-selektivni: CECXG; Negativni alosterni modulatori: RO4491533 |
Grupa III | Agonisti: Neselektivni: L-AP4; mGlu4-selektivni: PHCCC • VU-001,171 • VU-0155,041; mGlu7-selektivni: AMN082; mGlu8-selektivni: DCPG Antagonisti: Neselektivni: CPPG • MAP4 • MSOP • MPPG • MTPG • UBP-1112; mGlu7-selektivni: MMPIP |
transporta
EAAT | |
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vGluT |