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LY-379,268

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LY-379,268
Identifiers
  • (1S,2R,5R,6R)-2-amino-4-oxabicyclo[3.1.0]hexane-2,6-dicarboxylic acid
CAS Number
PubChemCID
ChemSpider
UNII
ChEBI
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC7H9NO5
Molar mass187.151g·mol−1
3D model (JSmol)
  • C1[C@]([C@@H]2[C@H]([C@@H]2O1)C(=O)O)(C(=O)O)N
  • InChI=1S/C7H9NO5/c8-7(6(11)12)1-13-4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1☒N
  • Key:YASVRZWVUGJELU-MDASVERJSA-N☒N
☒NcheckY(what is this?)(verify)

LY-379,268is a drug that is used in neuroscience research, which acts as a potent and selective agonist for the group II metabotropic glutamate receptors (mGluR2/3).

It is derived from the older mGluR group II agonisteglumegad,[1]and led on to the development of the more potent compoundLY-404,039,[2]but is still widely used in research itself. LY-379,268 hassedative,neuroprotective,anti-addictive andanticonvulsanteffects in animals,[3][4][5]and blocks the effects ofPCPandDOI,[6][7][8][9][10]which has led to research into LY-379,268 and similar compounds asantipsychoticdrugs for the treatment ofschizophreniain animals.[11][12]

There are inconsistent findings about an additional activity as adopamine D2 receptorpartial agonist.[13][14]

See also

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References

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  1. ^Monn JA, Valli MJ, Massey SM, Hansen MM, Kress TJ, Wepsiec JP, et al. (March 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".Journal of Medicinal Chemistry.42(6): 1027–1040.doi:10.1021/jm980616n.PMID10090786.
  2. ^Rorick-Kehn LM, Johnson BG, Burkey JL, Wright RA, Calligaro DO, Marek GJ, et al. (April 2007). "Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039)".The Journal of Pharmacology and Experimental Therapeutics.321(1): 308–317.doi:10.1124/jpet.106.110809.PMID17204749.S2CID23666836.
  3. ^Cai Z, Xiao F, Fratkin JD, Rhodes PG (December 1999). "Protection of neonatal rat brain from hypoxic-ischemic injury by LY379268, a Group II metabotropic glutamate receptor agonist".NeuroReport.10(18): 3927–3931.doi:10.1097/00001756-199912160-00037.PMID10716235.
  4. ^Moldrich RX, Jeffrey M, Talebi A, Beart PM, Chapman AG, Meldrum BS (July 2001). "Anti-epileptic activity of group II metabotropic glutamate receptor agonists (--)-2-oxa-4-aminobicyclo[3.1.0]hexane-4,6-dicarboxylate (LY379268) and (--)-2-thia-4-aminobicyclo[3.1.0]hexane-4,6-dicarboxylate (LY389795)".Neuropharmacology.41(1): 8–18.doi:10.1016/S0028-3908(01)00044-2.PMID11445181.S2CID26104177.
  5. ^Uys JD, LaLumiere RT (November 2008). "Glutamate: the new frontier in pharmacotherapy for cocaine addiction".CNS & Neurological Disorders Drug Targets.7(5): 482–491.doi:10.2174/187152708786927868.PMID19128205.
  6. ^Cartmell J, Monn JA, Schoepp DD (March 2000). "Attenuation of specific PCP-evoked behaviors by the potent mGlu2/3 receptor agonist, LY379268 and comparison with the atypical antipsychotic, clozapine".Psychopharmacology.148(4): 423–429.doi:10.1007/s002130050072.PMID10928316.S2CID22988081.
  7. ^Greenslade RG, Mitchell SN (July 2004). "Selective action of (-)-2-oxa-4-aminobicyclo[3.1.0]hexane-4,6-dicarboxylate (LY379268), a group II metabotropic glutamate receptor agonist, on basal and phencyclidine-induced dopamine release in the nucleus accumbens shell".Neuropharmacology.47(1): 1–8.doi:10.1016/j.neuropharm.2004.02.015.PMID15165829.S2CID25267021.
  8. ^Kłodzinska A, Bijak M, Tokarski K, Pilc A (September 2002). "Group II mGlu receptor agonists inhibit behavioural and electrophysiological effects of DOI in mice".Pharmacology, Biochemistry, and Behavior.73(2): 327–332.doi:10.1016/S0091-3057(02)00845-6.PMID12117586.S2CID28841684.
  9. ^Molinaro G, Traficante A, Riozzi B, Di Menna L, Curto M, Pallottino S, et al. (August 2009). "Activation of mGlu2/3 metabotropic glutamate receptors negatively regulates the stimulation of inositol phospholipid hydrolysis mediated by 5-hydroxytryptamine2A serotonin receptors in the frontal cortex of living mice".Molecular Pharmacology.76(2): 379–387.doi:10.1124/mol.109.056580.PMID19439499.S2CID14722003.
  10. ^Engel M,Snikeris P, Matosin N, Newell KA, Huang XF, Frank E (April 2016)."mGluR2/3 agonist LY379268 rescues NMDA and GABAA receptor level deficits induced in a two-hit mouse model of schizophrenia".Psychopharmacology.233(8): 1349–1359.doi:10.1007/s00213-016-4230-0.PMID26861891.S2CID253744752.
  11. ^Carter K, Dickerson J, Schoepp DD, Reilly M, Herring N, Williams J, et al. (December 2004). "The mGlu2/3 receptor agonist LY379268 injected into cortex or thalamus decreases neuronal injury in retrosplenial cortex produced by NMDA receptor antagonist MK-801: possible implications for psychosis".Neuropharmacology.47(8): 1135–1145.doi:10.1016/j.neuropharm.2004.08.018.PMID15567423.S2CID22374384.
  12. ^Imre G (2007)."The preclinical properties of a novel group II metabotropic glutamate receptor agonist LY379268".CNS Drug Reviews.13(4): 444–464.doi:10.1111/j.1527-3458.2007.00024.x.PMC6494167.PMID18078428.
  13. ^Seeman P, Guan HC (November 2008). "Phencyclidine and glutamate agonist LY379268 stimulate dopamine D2High receptors: D2 basis for schizophrenia".Synapse.62(11): 819–828.doi:10.1002/syn.20561.PMID18720422.S2CID206519749.
  14. ^Fell MJ, Perry KW, Falcone JF, Johnson BG, Barth VN, Rash KS, et al. (December 2009). "In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268)".The Journal of Pharmacology and Experimental Therapeutics.331(3): 1126–1136.doi:10.1124/jpet.109.160598.PMID19755662.S2CID23981819.
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