• Corpus ID: 45961850

Pharmacological profile of NPC 12626, a novel, competitive N-methyl-D-aspartate receptor antagonist.

  title={Pharmacological profile of NPC 12626, a novel, competitive N-methyl-D-aspartate receptor antagonist.},
  author={John Wm. Ferkany and Donald J. Kyle and J M Willets and Waclaw J. Rzeszotarski and M. E. Guzewska and Suzanne R. Ellenberger and S. M. Jones and Aida I. Sacaan and Lawrence D. Snell and Susan A. Borosky},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={250 1},
  • J. Ferkany, D. Kyle, S. Borosky
  • Published 1 July 1989
  • Biology, Chemistry
  • The Journal of pharmacology and experimental therapeutics
The novel compound 2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid (NPC 12626) was evaluated for activity in a variety of tests associated with receptors for excitatory amino acids. NPC 12626 failed to inhibit the specific binding of RS-[3H] amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid or [3H] kainic acid to brain membranes in vitro but displaced both agonist and antagonist binding to N-methyl-D-aspartic acid (NMDA) receptors. Like cis-(+/-)-3-(2-carboxypiperazine-4-yl)propyl-1… 
Drug discrimination based on the competitive N-methyl-d-aspartate antagonist, NPC 12626
The data indicate that the discriminative stimulus properties of NPC 12626 are selective and shared by CPP but not by phencyclidine, pentobarbital or NMDA, which suggests that competitive antagonists such as NPC12626 and CPP may not have Phencyclidine-like abuse liability.
Sites for antagonism on the N-methyl-D-aspartate receptor channel complex.
  • E. Wong, J. Kemp
  • Biology
    Annual review of pharmacology and toxicology
  • 1991
This approach has been very fruitful in the characterization of various sites associated with the NMDA receptor chan­ nel complex, and has complemented the powerful electrophysiological power of these amino acids in the mammalian central nervous system.
Neuroprotectant effects of LY 274614, a structurally novel systemically active competitive NMDA receptor antagonist
In adult rats, the neuro-degenerative effects following the intrastriatal infusions of NMDA or quinolinate, but not kainate, were prevented by LY 274614 and is a promising therapeutic agent for conditions where glutamate plays a role in the pathology of neuronal degeneration.
Quantitative structure activity relationship (QSAR) of competitive N-methyl-D-aspartate (NMDA) antagonists
By the quantitative structure activity relationship (QSAR) model developed here, it is possible to predict the activity of a potent drug before its synthesis since only theoretically determined molecular parameters are used for the prediction.