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词条 Besonprodil
释义

  1. References

{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 459976920
| IUPAC_name = 6-[2-(4-[(4-fluorophenyl)methyl]piperidin-1-yl)ethylsulfinyl]-3H-1,3-benzoxazol-2-one
| image = Besonprodil.svg
| width = 325
| tradename =
| pregnancy_AU =
| pregnancy_US =
| pregnancy_category =
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US =
| legal_status =
| bioavailability =
| protein_bound =
| metabolism =
| excretion =
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 253450-09-8
| ATC_prefix = None
| ATC_suffix =
| PubChem = 156328
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 137662
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 5K3N2D15WW
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 219631
| synonyms = CI-1041
| C=21 | H=23 | F=1 | N=2 | O=3 | S=1
| molecular_weight = 402.481 g/mol
| smiles = c4cc(F)ccc4CC(CC2)CCN2CCS(=O)c(cc1o3)ccc1[nH]c3=O
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = FCBQJNCAKZSIAH-UHFFFAOYSA-N
}}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

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

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