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==External links==
==External links==
*{{cite web | url = http://www.iuphar-db.org/PRODGPCR/ReceptorDisplayForward?receptorID=2272 | title = Metabotropic Glutamate Receptors: mGlu<sub>3</sub> | accessdate = | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
*{{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2272 | title = Metabotropic Glutamate Receptors: mGlu<sub>3</sub> | accessdate = | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}


==Further reading==
==Further reading==

Revision as of 15:33, 5 December 2008

Template:PBB Glutamate receptor, metabotropic 3, also known as GRM3, is a human gene.[1]

Template:PBB Summary

Ligands

Though truly GluR3 selective agents still await their discovery, mixed GluR2/3 (group-II) ligands with selectivity over other GluR-subtypes are known (2008). Low oral bioavailability is observed in some of them, but it can be met by applying a prodrug strategy.[2] Non-glutamatergic characteristics can not completely be excluded: an additional D2 dopaminergic component was found for LY-354,740 and LY-379,268.[3]

Agonists

  • with a bicyclo[3.1.0]hexane skeleton
  • (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid[9]

Antagonists

  • LY-341,495 and its 1-fluoro analog[10]: potent orthosteric antagonists
  • MGS-0039[11], HYDIA[12] (both with bicyclo[3.1.0]hexane skeleton)

Allosteric modulators

  • MNI-137[13]: inhibitior
  • compound 7p[14]: non-competitive antagonist (presumably allosteric inhibitor)

See also

References

  1. ^ "Entrez Gene: GRM3 glutamate receptor, metabotropic 3".
  2. ^ Rorick-Kehn LM, Perkins EJ, Knitowski KM; et al. (2006). "Improved bioavailability of the mGlu2/3 receptor agonist LY354740 using a prodrug strategy: in vivo pharmacology of LY544344". J. Pharmacol. Exp. Ther. 316 (2): 905–13. doi:10.1124/jpet.105.091926. PMID 16223873. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  3. ^ Seeman P, Caruso C, Lasaga M (2008). "Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268". Synapse. 62 (2): 154–8. doi:10.1002/syn.20482. PMID 18000815.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  4. ^ Nakazato A, Kumagai T, Sakagami K; et al. (2000). "Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists". J. Med. Chem. 43 (25): 4893–909. PMID 11123999. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  5. ^ Monn JA, Massey SM, Valli MJ; et al. (2007). "Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors". J. Med. Chem. 50 (2): 233–40. doi:10.1021/jm060917u. PMID 17228865. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  6. ^ Monn JA, Valli MJ, Massey SM; et al. (1999). "Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors". J. Med. Chem. 42 (6): 1027–40. doi:10.1021/jm980616n. PMID 10090786. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  7. ^ Monn JA, Valli MJ, Massey SM; et al. (1997). "Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties". J. Med. Chem. 40 (4): 528–37. doi:10.1021/jm9606756. PMID 9046344. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  8. ^ Dominguez C, Prieto L, Valli MJ; et al. (2005). "Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist". J. Med. Chem. 48 (10): 3605–12. doi:10.1021/jm040222y. PMID 15887967. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  9. ^ Clausen RP, Bräuner-Osborne H, Greenwood JR; et al. (2002). "Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid". J. Med. Chem. 45 (19): 4240–5. PMID 12213064. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  10. ^ Sakagami K, Yasuhara A, Chaki S; et al. (2008). "Synthesis, in vitro pharmacology, and pharmacokinetic profiles of 2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic acid and its 6-heptyl ester, a potent mGluR2 antagonist". Bioorg. Med. Chem. 16 (8): 4359–66. doi:10.1016/j.bmc.2008.02.066. PMID 18348906. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  11. ^ a) Nakazato A, Sakagami K, Yasuhara A; et al. (2004). "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". J. Med. Chem. 47 (18): 4570–87. doi:10.1021/jm0400294. PMID 15317467. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link),
    b) Yasuhara A, Nakamura M, Sakagami K; et al. (2006). "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". Bioorg. Med. Chem. 14 (12): 4193–207. doi:10.1016/j.bmc.2006.01.060. PMID 16487713. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link),
    c) Yasuhara A, Sakagami K, Yoshikawa R, Chaki S, Nakamura M, Nakazato A (2006). "Synthesis, in vitro pharmacology, and structure-activity relationships of 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as mGluR2 antagonists". Bioorg. Med. Chem. 14 (10): 3405–20. doi:10.1016/j.bmc.2005.12.061. PMID 16431115.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  12. ^ Woltering TJ, Adam G, Huguenin P; et al. (2008). "Asymmetric synthesis and receptor pharmacology of the group II mGlu receptor ligand (1S,2R,3R,5R,6S)-2-amino-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid-HYDIA". ChemMedChem. 3 (2): 323–35. doi:10.1002/cmdc.200700226. PMID 18058780. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  13. ^ Hemstapat K, Da Costa H, Nong Y; et al. (2007). "A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors". J. Pharmacol. Exp. Ther. 322 (1): 254–64. doi:10.1124/jpet.106.117093. PMID 17416742. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  14. ^ Woltering TJ, Wichmann J, Goetschi E; et al. (2008). "Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists". Bioorg. Med. Chem. Lett. 18 (8): 2725–9. doi:10.1016/j.bmcl.2008.02.076. PMID 18374569. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)

Further reading

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