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Fanapanel

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Fanapanel
Skeletal formula
Space-filling model of fanapanel as an anion
Clinical data
ATC code
  • None
Identifiers
  • {[7-(4-Morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydro-1(2H)-quinoxalinyl]methyl}phosphonic acid
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC14H15F3N3O6P
Molar mass409.258 g·mol−1
3D model (JSmol)
  • c1c(c(cc2c1[nH]c(=O)c(=O)n2CP(=O)(O)O)N3CCOCC3)C(F)(F)F
  • InChI=1S/C14H15F3N3O6P/c15-14(16,17)8-5-9-11(6-10(8)19-1-3-26-4-2-19)20(7-27(23,24)25)13(22)12(21)18-9/h5-6H,1-4,7H2,(H,18,21)(H2,23,24,25)
  • Key:WZMQMKNCWDCCMT-UHFFFAOYSA-N

Fanapanel (INN, code nameZK-200775), also known asMPQX, is aquinoxalinedionederivativedrug which acts as acompetitive antagonist of theAMPA receptor.[1] It was under development bySchering AG for the treatment ofcerebral ischemia associated withstroke andtrauma, butclinical trials were halted for safety reasons related to possibleglial cell toxicity and due to intolerableside effects such as excessivesedation, reduction inconsciousness (consisting ofstupor andcoma), and transientneurological deterioration.[2][3] The drug was also observed to producevisual alteration and impairment, includingblurred vision, strongly impairedcolor perception, and reducedvisual acuity anddark vision, side effects thought to be caused by blockade of AMPA receptors in theretina.[4]

References

[edit]
  1. ^Turski L, Huth A, Sheardown M, McDonald F, Neuhaus R, Schneider HH, et al. (September 1998)."ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma".Proceedings of the National Academy of Sciences of the United States of America.95 (18):10960–10965.Bibcode:1998PNAS...9510960T.doi:10.1073/pnas.95.18.10960.PMC 28003.PMID 9724812.
  2. ^Walters MR, Kaste M, Lees KR, Diener HC, Hommel M, De Keyser J, et al. (2005). "The AMPA antagonist ZK 200775 in patients with acute ischaemic stroke: a double-blind, multicentre, placebo-controlled safety and tolerability study".Cerebrovascular Diseases.20 (5):304–309.doi:10.1159/000087929.PMID 16131799.S2CID 25034903.
  3. ^Elting JW, Sulter GA, Kaste M, Lees KR, Diener HC, Hommel M, et al. (December 2002)."AMPA antagonist ZK200775 in patients with acute ischemic stroke: possible glial cell toxicity detected by monitoring of S-100B serum levels".Stroke.33 (12):2813–2818.doi:10.1161/01.str.0000043823.37955.fb.PMID 12468775.
  4. ^Bergholz R, Staks T, Rüther K (August 2010)."Effects of the AMPA antagonist ZK 200775 on visual function: a randomized controlled trial".PLOS ONE.5 (8): e12111.Bibcode:2010PLoSO...512111B.doi:10.1371/journal.pone.0012111.PMC 2920815.PMID 20711429.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor
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