Besonprodil

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Besonprodil
Besonprodil structure.png
Systematic (IUPAC) name
6-[2-(4-[(4-fluorophenyl)methyl]piperidin-1-yl)ethylsulfinyl]-3H-1,3-benzoxazol-2-one
Clinical data
Legal status
?
Identifiers
CAS number 253450-09-8 N
ATC code None
PubChem CID 156328
ChemSpider 137662 YesY
UNII 5K3N2D15WW YesY
ChEMBL CHEMBL219631 YesY
Synonyms Besonprodil, CI-1041
Chemical data
Formula C21H23FN2O3S 
Mol. mass 402.481 g/mol
 N (what is this?)  (verify)

Besonprodil (CI-1041) is a drug which acts as an NMDA antagonist, selective for the NR2B subunit.[1][2] It is under development as a supplemental medication for Parkinson's disease, and has been shown in animals to be effective in counteracting the dyskinesias associated with long term treatment with levodopa 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. 
  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. 
  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 : Official Journal of the Movement Disorder Society 21 (1): 9–17. doi:10.1002/mds.20654. PMID 16127720. 
  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. 
  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 : MN 38 (2): 128–42. doi:10.1007/s12031-008-9137-8. PMID 18704766. 
  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. 
  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.