MGS-0039

In today's world, MGS-0039 is a topic that generates great interest and debate in society. From its origins to the present, MGS-0039 has been a point of reference and discussion in different areas, from politics to culture. Its impact has been such that it has left an indelible mark on history, and its relevance endures to this day. In this article, we will explore the various facets of MGS-0039, from its most controversial aspects to its positive contributions. We will analyze its influence in different areas and how it has shaped the world in which we live. Without a doubt, MGS-0039 continues to be a topic of great importance and its study is essential to understand today's society.

MGS-0039
Clinical data
ATC code
  • None
Legal status
Legal status
  • In general: non-regulated
Identifiers
  • (1R,2R,3R,5R,6R)-2-amino-3-(3,4-dichlorobenzyloxy)-6-fluorobicyclohexane-2,6-dicarboxylic acid
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H14Cl2NO5
Molar mass359.18 g·mol−1
3D model (JSmol)
  • F2(C(=O)O)3(C(=O)O)(N)(OCc1ccc(Cl)c(Cl)c1)C23
  • InChI=1S/C15H14Cl2FNO5/c16-8-2-1-6(3-9(8)17)5-24-10-4-7-11(14(7,18)12(20)21)15(10,19)13(22)23/h1-3,7,10-11H,4-5,19H2,(H,20,21)(H,22,23)/t7-,10-,11+,14-,15+/m1/s1
  • Key:LFAGGDAZZKUVKO-JAGWWQSPSA-N

MGS-0039 is a drug that is used in neuroscientific research, which acts as a potent and selective antagonist for group II of the metabotropic glutamate receptors (mGluR2/3).[1][2] It produces antidepressant and anxiolytic effects in animal studies,[3][4][5][6] and has been shown to boost release of dopamine and serotonin in specific brain areas.[7][8] Research has suggested this may occur through a similar mechanism as that suggested for the similarly glutamatergic drug ketamine.[9][10]

References

  1. ^ Chaki S, Yoshikawa R, Hirota S, Shimazaki T, Maeda M, Kawashima N, et al. (March 2004). "MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity". Neuropharmacology. 46 (4): 457–67. doi:10.1016/j.neuropharm.2003.10.009. PMID 14975669. S2CID 40533560.
  2. ^ Nakazato A, Sakagami K, Yasuhara A, Ohta H, Yoshikawa R, Itoh M, et al. (August 2004). "Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclohexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists". Journal of Medicinal Chemistry. 47 (18): 4570–87. doi:10.1021/jm0400294. PMID 15317467.
  3. ^ Shimazaki T, Iijima M, Chaki S (October 2004). "Anxiolytic-like activity of MGS0039, a potent group II metabotropic glutamate receptor antagonist, in a marble-burying behavior test". European Journal of Pharmacology. 501 (1–3): 121–5. doi:10.1016/j.ejphar.2004.08.016. PMID 15464070.
  4. ^ Yasuhara A, Nakamura M, Sakagami K, Shimazaki T, Yoshikawa R, Chaki S, et al. (June 2006). "Prodrugs of 3-(3,4-dichlorobenzyloxy)-2-amino-6-fluorobicyclohexane-2,6-dicarboxylic acid (MGS0039): a potent and orally active group II mGluR antagonist with antidepressant-like potential". Bioorganic & Medicinal Chemistry. 14 (12): 4193–207. doi:10.1016/j.bmc.2006.01.060. PMID 16487713.
  5. ^ Yoshimizu T, Shimazaki T, Ito A, Chaki S (July 2006). "An mGluR2/3 antagonist, MGS0039, exerts antidepressant and anxiolytic effects in behavioral models in rats". Psychopharmacology. 186 (4): 587–93. doi:10.1007/s00213-006-0390-7. PMID 16612616. S2CID 7801709.
  6. ^ Stachowicz K, Wierońska J, Domin H, Chaki S, Pilc A (2011). "Anxiolytic-like activity of MGS0039, a selective group II mGlu receptor antagonist, is serotonin- and GABA-dependent". Pharmacological Reports. 63 (4): 880–7. doi:10.1016/S1734-1140(11)70603-X. PMID 22001975.
  7. ^ Kawashima N, Karasawa J, Shimazaki T, Chaki S, Okuyama S, Yasuhara A, Nakazato A (April 2005). "Neuropharmacological profiles of antagonists of group II metabotropic glutamate receptors". Neuroscience Letters. 378 (3): 131–4. doi:10.1016/j.neulet.2004.12.021. PMID 15781145. S2CID 26509964.
  8. ^ Karasawa J, Yoshimizu T, Chaki S (January 2006). "A metabotropic glutamate 2/3 receptor antagonist, MGS0039, increases extracellular dopamine levels in the nucleus accumbens shell". Neuroscience Letters. 393 (2–3): 127–30. doi:10.1016/j.neulet.2005.09.058. PMID 16233956. S2CID 20736438.
  9. ^ Pałucha-Poniewiera A, Wierońska JM, Brański P, Stachowicz K, Chaki S, Pilc A (December 2010). "On the mechanism of the antidepressant-like action of group II mGlu receptor antagonist, MGS0039". Psychopharmacology. 212 (4): 523–35. doi:10.1007/s00213-010-1978-5. PMC 2981731. PMID 20703449.
  10. ^ Koike H, Iijima M, Chaki S (December 2011). "Involvement of the mammalian target of rapamycin signaling in the antidepressant-like effect of group II metabotropic glutamate receptor antagonists". Neuropharmacology. 61 (8): 1419–23. doi:10.1016/j.neuropharm.2011.08.034. PMID 21903115. S2CID 23923192.