Besonprodil

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]

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
PubChem CID
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)

References
  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.


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