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L-687,414

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Pharmaceutical compound
L-687,414
Clinical data
Other namesL-687414; L687414; cis-4-Methyl-HA-966
Drug classGlycine-site NMDA receptor antagonist or very weak partial agonist
Identifiers
IUPAC name
  • (3S,4S)-3-amino-1-hydroxy-4-methylpyrrolidin-2-one
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC5H10N2O2
Molar mass130.147 g·mol
3D model (JSmol)
SMILES
  • C1CN(C(=O)1N)O
InChI
  • InChI=1S/C5H10N2O2/c1-3-2-7(9)5(8)4(3)6/h3-4,9H,2,6H2,1H3/t3-,4-/m0/s1
  • Key:SKYSFPFYQBZGDC-IMJSIDKUSA-N

L-687,414 is a glycine-site NMDA receptor antagonist or low-efficacy partial agonist (EmaxTooltip maximal efficacy ≈ 10%) which is used in scientific research. It a close analogue of HA-966. The drug has been found to produce hyperlocomotion (a psychostimulant-like effect), analgesia or antinociceptive effects, anticonvulsant effects, and neuroprotective effects in animals. In contrast to uncompetitive NMDA receptor antagonists like ketamine and phencyclidine (PCP), L-687,414 has not been associated with the development of brain vacuoles (i.e., Olney's lesions) in animals.

Trace amine-associated receptor 1 (TAAR1) partial and full agonists, including RO5166017, RO5203648, RO5256390, and RO5263397, have been found to reverse the hyperlocomotion induced by L-687,414 as well as by other NMDA receptor antagonists like PCP in rodents. Similarly, glycine transporter 1 (GlyT1) inhibitors reverse the hyperlocomotion induced by L-687,414 in rodents. As such, TAAR1 agonists and GlyT1 inhibitors may have antipsychotic-like properties.

References

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Ionotropic glutamate receptor modulators
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor


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