| Identification | Back Directory | [Name]
LY 379268 | [CAS]
191471-52-0 | [Synonyms]
CS-1087
LY397268
LY 379268
(1R,4R,5S,6R)-4-Amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylicacid
2-Oxabicyclo[3.1.0]hexane-4,6-dicarboxylicacid,4-amino-,(1R,4R,5S,6R)- | [Molecular Formula]
C7H9NO5 | [MDL Number]
MFCD11100365 | [MOL File]
191471-52-0.mol | [Molecular Weight]
187.15 |
| Chemical Properties | Back Directory | [Boiling point ]
413.9±45.0 °C(Predicted) | [density ]
1.716±0.06 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
Soluble in H2O or NaOH | [form ]
solid | [pka]
1.81±0.40(Predicted) | [color ]
White | [Water Solubility ]
Soluble to 20 mM in water and to 100 mM in 1eq. NaOH |
| Hazard Information | Back Directory | [Uses]
LY 379268 is a group II metabotropic glutamate receptors (mGlu2/3) receptor agonist (1,2). Studies have shown that LY379268 significantly attenuated cocaine-induced increases in DA in nonhuman primates. | [Definition]
ChEBI: LY 379268 is an organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia. It has a role as a metabotropic glutamate receptor agonist, a neuroprotective agent, an antipsychotic agent and an anxiolytic drug. It is an organic heterobicyclic compound, a bridged compound and an amino dicarboxylic acid. | [Biological Activity]
Highly selective group II mGlu receptor agonist (EC 50 values are 2.69 and 4.48 nM for hmGlu 2 and hmGlu 3 respectively) that displays > 80-fold selectivity over group I and group III receptors. Provides protection against NMDA-mediated cell death in vitro and offers almost complete protection against CA1 hippocampal damage following global ischemia in gerbils. Orally and systemically active. | [in vivo]
For LY379268, when a 3?mg/kg dose is given prior to an intraplantar injection of carrageenan, the inflammatory hyperalgesia that developed is significantly delayed, without affecting the inflammation of the paw[2].
In a model of mouse tail withdrawal to warm water, LY379268 (12?mg/kg; i.p.), given before a subcutaneous tail injection of capsaicin, reduces the subsequent neurogenic hyperalgesia[2]. | [IC 50]
hmGluR2: 2.69 nM (EC50); hmGluR3: 4.48 nM (EC50); hmGluR2: 14.1 nM (Ki); hmGluR3: 5.8 nM (Ki) | [storage]
Store at +4°C |
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