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