Sarizotan

Sarizotan
(IUPAC) ime
1-[(2R)-3,4-dihidro-2H-hromen-2-il]-N-([5-(4-fluorofenil)pyridin-3-il]metil)metanamin
Klinički podaci
Identifikatori
CAS broj 177975-08-5
ATC kod nije dodeljen
PubChem[1][2] 6918388
ChemSpider[3] 2319847
UNII 467LU0UCUW DaY
Hemijski podaci
Formula C22H21FN2O 
Mol. masa 348,413 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

Sarizotan (EMD-128,130) je selektivni agonist 5-HT1A receptor i antagonist D2 receptora,[4] sa antipsihotičkim dejstvom.[5][6] Takođe je poznato da redukuje diskineziju kod dugotrajnih tretmana Parkinsonove bolesti sa levodopom.[7][8][9][10]

Reference

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ 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. DOI:10.1177/026988110201600301. PMID 12236624. 
  5. ↑ 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. DOI:10.1124/jpet.105.087163. PMID 15987834. 
  6. ↑ 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. DOI:10.1007/s00213-007-0762-7. PMID 17393144. 
  7. ↑ 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. 
  8. ↑ 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. DOI:10.1007/s00702-003-0094-7. PMID 14767715. 
  9. ↑ 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. DOI:10.1002/mds.20370. PMID 15791634. 
  10. ↑ 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. DOI:10.1016/j.parkreldis.2008.11.001. PMID 19196540. 

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