Sarizotan
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]
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| IUPAC ime | |
|---|---|
1-[(2R)-3,4-dihidro-2H-hromen-2-il]-N-([5-(4-fluorofenil)pyridin-3-il]metil)metanamin | |
| Klinički podaci | |
| Kategorija trudnoće |
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| Način primene | Oralno |
| Identifikatori | |
| CAS broj | 177975-08-5  |
| ATC kod | none |
| PubChem | CID 6918388 |
| ChemSpider | 2319847 |
| UNII | 467LU0UCUW |
| Hemijski podaci | |
| Formula | C22H21FN2O |
| Molarna masa | 348,413 g/mol |
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Reference
уреди- ^ 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.}
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
