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Sarizotan Reference Vidi još Spoljašnje veze Мени за навигацију177975-08-569183882319847467LU0UCUW1223662410.1177/0269881102016003011598783410.1124/jpet.105.0871631739314410.1007/s00213-007-0762-7117232721476771510.1007/s00702-003-0094-71579163410.1002/mds.203701919654010.1016/j.parkreldis.2008.11.001ууу

АминиПиридиниОрганофлуоридиХромани


selektivniagonist5-HT1A receptorantagonistD2 receptoraantipsihotičkimdiskinezijuParkinsonove bolestilevodopomAzaperonBenperidolBromperidolDroperidolFluanizonHaloperidolLenperonMoperonPipamperonSpiperonTimiperonTrifluperidolKlopimozidFluspirilenPenfluridolPimozidAcepromazinAcetofenazinButaperazinKarfenazinHloracizinHlorproetazinHlorpromazinCijamemazinDiksirazinFluacizinFlufenazinLevomepromazin/MetotrimeprazinMezoridazinPerazinPericijazinPerfenazinPiperacetazinPipotiazinProhlorperazinPromazinPrometazinPropiomazinSulforidazinTietilperazinTiopropazatTioproperazinTioridazinTrifluoperazinTriflupromazinHlorprotiksenKlopentiksolFlupentiksolTiotiksenZuklopentiksolButaklamolFluotracenLoksapinTrimipraminCinuperonMelperonSetoperonIloperidonOkaperidonPaliperidonRisperidonLurasidonePerospironRevospironTiospironZiprasidonAmperozidAripiprazolBifeprunoksBrekspiprazolElopiprazolUmespironAmoksapinAsenapinKarpipraminKlocapraminKlorotepinKlotiapinKlozapinFluperlapinGevotrolinMetitepinMosapraminNDMCOlanzapinPihindonKvetijapinTenilapinZotepinWHO-EMPovučeniKlinička ispitivanjaFaza IIINije dospeo do faze IIIMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6D










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Sarizotan




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Sarizotan
Sarizotan.png

IUPAC ime
1-[(2R)-3,4-dihidro-2H-hromen-2-il]-N-([5-(4-fluorofenil)pyridin-3-il]metil)metanamin
Klinički podaci
Kategorija trudnoće

  • N/A
Način primeneOralno
Identifikatori
CAS broj
177975-08-5 ДаY
ATC kodnone
PubChemCID 6918388
ChemSpider2319847
UNII
467LU0UCUW ДаY
Hemijski podaci
Formula
C22H21FN2O
Molarna masa348,413 g/mol



Sarizotan (EMD-128,130) je selektivni agonist 5-HT1A receptor i antagonist D2 receptora,[1] sa antipsihotičkim dejstvom.[2][3] Takođe je poznato da redukuje diskineziju kod dugotrajnih tretmana Parkinsonove bolesti sa levodopom.[4][5][6][7]



Reference




  1. ^ Rabiner, E. A.; Gunn, R. N.; Wilkins, M. R.; Sedman, E.; Grasby, P. M. (2002). „Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with 11CWAY-100635 and 11Craclopride”. Journal of psychopharmacology (Oxford, England). 16 (3): 195—199. PMID 12236624. doi:10.1177/026988110201600301. }


  2. ^ Assié, M.; Ravailhe, V.; Faucillon, V.; Newman-Tancredi, A. (2005). „Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain”. The Journal of Pharmacology and Experimental Therapeutics. 315 (1): 265—272. PMID 15987834. doi:10.1124/jpet.105.087163. 


  3. ^ Auclair, A.; Galinier, A.; Besnard, J.; Newman-Tancredi, A.; Depoortère, R. (2007). „Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats”. Psychopharmacology. 193 (1): 45—54. PMID 17393144. doi:10.1007/s00213-007-0762-7. 


  4. ^ Bibbiani, F.; Oh, J. D.; Chase, T. N. (2001). „Serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models”. Neurology. 57 (10): 1829—1834. PMID 11723272. 


  5. ^ Bartoszyk, G.; Van Amsterdam, C.; Greiner, H.; Rautenberg, W.; Russ, H.; Seyfried, C. (2004). „Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile”. Journal of neural transmission (Vienna, Austria : 1996). 111 (2): 113—126. PMID 14767715. doi:10.1007/s00702-003-0094-7. 


  6. ^ Bara-Jimenez, W.; Bibbiani, F.; Morris, M.; Dimitrova, T.; Sherzai, A.; Mouradian, M.; Chase, T. (2005). „Effects of serotonin 5-HT1A agonist in advanced Parkinson's disease”. Movement disorders : official journal of the Movement Disorder Society. 20 (8): 932—936. PMID 15791634. doi:10.1002/mds.20370. 


  7. ^ Grégoire, L.; Samadi, P.; Graham, J.; Bédard, P.; Bartoszyk, G.; Di Paolo, T. (2009). „Low doses of sarizotan reduce dyskinesias and maintain antiparkinsonian efficacy of L-Dopa in parkinsonian monkeys”. Parkinsonism & related disorders. 15 (6): 445—452. PMID 19196540. doi:10.1016/j.parkreldis.2008.11.001. 



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