L-687,414

Pharmaceutical compound From Wikipedia, the free encyclopedia

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.[1][2][3][4][5] It is a close analogue of HA-966.[5] The drug has been found to produce hyperlocomotion (a psychostimulant-like effect),[6][7] analgesia[4] or antinociceptive effects,[8][9] anticonvulsant effects,[2][6] and neuroprotective effects in animals.[10] 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.[11]

Other namesL-687414; L687414; cis-4-Methyl-HA-966
CAS Number
Quick facts Clinical data, Other names ...
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
  • (3S,4S)-3-amino-1-hydroxy-4-methylpyrrolidin-2-one
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC5H10N2O2
Molar mass130.147 g·mol−1
3D model (JSmol)
  • C[C@H]1CN(C(=O)[C@H]1N)O
  • 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
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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.[12][13][14][15][16] Similarly, glycine transporter 1 (GlyT1) inhibitors reverse the hyperlocomotion induced by L-687,414 in rodents.[17][7][18][19] As such, TAAR1 agonists and GlyT1 inhibitors may have antipsychotic-like properties.[12][17]

References

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