词条 | Besonprodil |
释义 |
| 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] References1. ^{{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=}} {{Ionotropic glutamate receptor modulators}}{{nervous-system-drug-stub}}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=}} 3 : NMDA receptor antagonists|Fluoroarenes|Piperidines |
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