Besonprodil

Besonprodil
Clinical data
Other names	CI-1041
ATC code	None;
Identifiers
	IUPAC name 6-[2-(4-[(4-fluorophenyl)methyl]piperidin-1-yl)ethylsulfinyl]-3H-1,3-benzoxazol-2-one;
CAS Number	253450-09-8 ;
PubChem CID	156328;
ChemSpider	137662 ;
UNII	5K3N2D15WW;
ChEMBL	ChEMBL219631 ;
CompTox Dashboard (EPA)	DTXSID2047270 ;
Chemical and physical data
Formula	C21H23FN2O3S
Molar mass	402.48 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c4cc(F)ccc4CC(CC2)CCN2CCS(=O)c(cc1o3)ccc1[nH]c3=O;
	InChI 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) ; Key:FCBQJNCAKZSIAH-UHFFFAOYSA-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

^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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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[pmid14654094-1] 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.

[pmid15135162-2] 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.

[pmid16127720-3] 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.

[pmid16739115-4] 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.

[pmid18704766-5] 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.

[pmid19576910-6] 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.

[pmid20303391-7] 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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