跳转到内容

L-687414

维基百科,自由的百科全书
L-687414
临床资料
其他名称L-687414; L687414; cis-4-Methyl-HA-966
药物类别Glycine-site NMDA receptor antagonist or very weak partial agonist
识别信息
  • (3S,4S)-3-amino-1-hydroxy-4-methylpyrrolidin-2-one
CAS号132695-96-6
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C5H10N2O2
摩尔质量130.15 g·mol−1
3D模型(JSmol英语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

L-687414是一种含氮有机化合物,化学式C
5
H
10
N
2
O
2
,可作为N-甲基-D-天门冬胺酸受体(NMDA受体)的拮抗剂[1][2],但其效能较低[3],只能算作部分激动剂[4],其同系物HA-966也是NMDA受体拮抗剂[5]

参考文献

[编辑]
  1. ^ Monaghan DT, Jane DE. Pharmacology of NMDA Receptors. Van Dongen AM (编). Biology of the NMDA Receptor. CRC Press/Taylor & Francis. 2009 [9 January 2025]. ISBN 978-1-4200-4414-0. PMID 21204415. 
  2. ^ Smith SE, Meldrum BS. The glycine-site NMDA receptor antagonist, R-(+)-cis-beta-methyl-3-amino-1-hydroxypyrrolid-2-one, L-687,414 is anticonvulsant in baboons. Eur J Pharmacol. January 1992, 211 (1): 109–111. PMID 1535595. doi:10.1016/0014-2999(92)90270-e. 
  3. ^ Grimwood S, Wilde GJ, Foster AC. Interactions between the glutamate and glycine recognition sites of the N-methyl-D-aspartate receptor from rat brain, as revealed from radioligand binding studies. J Neurochem. May 1993, 60 (5): 1729–1738. PMID 8097236. doi:10.1111/j.1471-4159.1993.tb13397.x. 
  4. ^ Laird JM, Mason GS, Webb J, Hill RG, Hargreaves RJ. Effects of a partial agonist and a full antagonist acting at the glycine site of the NMDA receptor on inflammation-induced mechanical hyperalgesia in rats. Br J Pharmacol. April 1996, 117 (7): 1487–1492. PMC 1909461可免费查阅. PMID 8730744. doi:10.1111/j.1476-5381.1996.tb15311.x. 
  5. ^ Priestley T, Marshall GR, Hill RG, Kemp JA. L-687,414, a low efficacy NMDA receptor glycine site partial agonist in vitro, does not prevent hippocampal LTP in vivo at plasma levels known to be neuroprotective. Br J Pharmacol. August 1998, 124 (8): 1767–1773. PMC 1565569可免费查阅. PMID 9756395. doi:10.1038/sj.bjp.0702010.