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PD-137889

From Wikipedia, the free encyclopedia
PD-137889
Names
IUPAC name
(4aR)-N-Methyl-1,2,3,4,9,9a-hexahydro-4aH-fluoren-4a-amine
Identifiers
3D model (JSmol)
ChemSpider
UNII
  • InChI=1S/C14H19N/c1-15-14-9-5-4-7-12(14)10-11-6-2-3-8-13(11)14/h2-3,6,8,12,15H,4-5,7,9-10H2,1H3
    Key: KQLIVVYSTDBTMZ-UHFFFAOYSA-N
  • c12c(cccc1)C3(NC)CCCCC3C2
Properties
C14H19N
Molar mass201.313 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

PD-137889 (N-methylhexahydrofluorenamine) is a chemical compound that is active as anNMDA receptor antagonist in thecentral nervous system at roughly 30 times the potency of the "flagship" of its class,ketamine,[1] and substitutes forphencyclidine in animal studies.[2][3][4] Ki [3H]TCP[a] binding = 27 nM versus ketamine's Ki = 860 nM.[5]

See also

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References

[edit]
  1. ^Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; Johnson, Graham; Lescosky, Leonard J.; Malone, Thomas C.; Michael, Andre (1993). "Synthesis and pharmacological evaluation of hexahydrofluorenamines as noncompetitive antagonists at the N-methyl-D-aspartate receptor".J Med Chem.36 (6):654–70.doi:10.1021/jm00058a002.PMID 8459395.
  2. ^Nicholson, Katherine L.; Balster, Robert L. (2003). "Evaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel blockers in rats".Psychopharmacology.170 (2):215–224.doi:10.1007/s00213-003-1527-6.PMID 2851738.S2CID 30803162.
  3. ^Bigge, Christopher F. (1993). "Structural requirements for the development of potent n-methyl-d-aspartic acid (NMDA) receptor antagonists".Biochemical Pharmacology.45 (8):1547–1561.doi:10.1016/0006-2952(93)90294-7.PMID 7683469.
  4. ^Bigge, Christopher F.; Malone, Thomas C. (1993). "Overview: Agonists, Antagonists and Modulators of the N-methyl-D-aspartic acid (NMDA) and α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) Subtypes of Glutamate Receptors".Current Opinion on Therapeutic Patents.3 (7):951–989.doi:10.1517/13543776.3.7.951.
  5. ^Polycyclic amine derivatives useful as cerebrovascular agentsArchived 2018-02-03 at theWayback Machine United States Patent; Coughenour, et al. Family ID: 22686445 Appl. #07/186,834
  1. ^[3H]N-[1-(2-thienyl)cyclohex-yl]piperidine
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor


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