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Besonprodil

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Besonprodil
Clinical data
Other namesCI-1041
ATC code
  • None
Identifiers
  • 6-[2-(4-[(4-fluorophenyl)methyl]piperidin-1-yl)ethylsulfinyl]-3H-1,3-benzoxazol-2-one
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC21H23FN2O3S
Molar mass402.48 g·mol−1
3D model (JSmol)
  • c4cc(F)ccc4CC(CC2)CCN2CCS(=O)c(cc1o3)ccc1[nH]c3=O
  • InChI=1S/C21H23FN2O3S/c22-17-3-1-15(2-4-17)13-16-7-9-24(10-8-16)11-12-28(26)18-5-6-19-20(14-18)27-21(25)23-19/h1-6,14,16H,7-13H2,(H,23,25) checkY
  • Key:FCBQJNCAKZSIAH-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Besonprodil (CI-1041) is a drug which acts as anNMDA antagonist, selective for theNR2B subunit.[1][2] It is under development as a supplemental medication forParkinson's disease, and has been shown in animals to be effective in counteracting thedyskinesias associated with long-term treatment withlevodopa and related drugs.[3][4][5][6][7]

References

[edit]
  1. ^Kovács G, Kocsis P, Tarnawa I, Horváth C, Szombathelyi Z, Farkas S (January 2004). "NR2B containing NMDA receptor dependent windup of single spinal neurons".Neuropharmacology.46 (1):23–30.doi:10.1016/S0028-3908(03)00339-3.PMID 14654094.S2CID 20562296.
  2. ^Barton ME, White HS (March 2004). "The effect of CGX-1007 and CI-1041, novel NMDA receptor antagonists, on kindling acquisition and expression".Epilepsy Research.59 (1):1–12.doi:10.1016/j.eplepsyres.2003.12.010.PMID 15135162.S2CID 23859984.
  3. ^Morissette M, Dridi M, Calon F, Hadj Tahar A, Meltzer LT, Bédard PJ, Di Paolo T (January 2006). "Prevention of levodopa-induced dyskinesias by a selective NR1A/2B N-methyl-D-aspartate receptor antagonist in parkinsonian monkeys: implication of preproenkephalin".Movement Disorders.21 (1):9–17.doi:10.1002/mds.20654.PMID 16127720.S2CID 34794881.
  4. ^Morissette M, Dridi M, Calon F, Hadj Tahar A, Meltzer LT, Bédard PJ, Di Paolo T (September 2006). "Prevention of dyskinesia by an NMDA receptor antagonist in MPTP monkeys: effect on adenosine A2A receptors".Synapse (New York, N.Y.).60 (3):239–50.doi:10.1002/syn.20295.PMID 16739115.S2CID 28098042.
  5. ^Ouattara B, Belkhir S, Morissette M, Dridi M, Samadi P, Grégoire L, Meltzer LT, Di Paolo T (June 2009). "Implication of NMDA receptors in the antidyskinetic activity of cabergoline, CI-1041, and Ro 61-8048 in MPTP monkeys with levodopa-induced dyskinesias".Journal of Molecular Neuroscience.38 (2):128–42.doi:10.1007/s12031-008-9137-8.PMID 18704766.S2CID 22646602.
  6. ^Tamim MK, Samadi P, Morissette M, Grégoire L, Ouattara B, Lévesque D, Rouillard C, Di Paolo T (January 2010)."Effect of non-dopaminergic drug treatment on Levodopa induced dyskinesias in MPTP monkeys: common implication of striatal neuropeptides".Neuropharmacology.58 (1):286–96.doi:10.1016/j.neuropharm.2009.06.030.PMID 19576910.S2CID 46331408.
  7. ^Ouattara B, Hoyer D, Grégoire L, Morissette M, Gasparini F, Gomez-Mancilla B, Di Paolo T (June 2010). "Changes of AMPA receptors in MPTP monkeys with levodopa-induced dyskinesias".Neuroscience.167 (4):1160–7.doi:10.1016/j.neuroscience.2010.03.022.PMID 20303391.S2CID 40680667.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor


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