Pimavanserin

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Pimavanserin
(IUPAC) ime
N-(4-fluorofenilmetil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloksi)fenilmetil)karbamid
Klinički podaci
Identifikatori
CAS broj 706779-91-1
706782-28-7 (tartarat)
ATC kod nije dodeljen
PubChem[1][2] 10071196
UNII JZ963P0DIK YesY
Hemijski podaci
Formula C25H34FN3O2 
Mol. masa 427,553 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

Pimavanserin (ACP-103) je lek koji deluje kao inverzni agonist na serotoninskom receptoru 5-HT2A, sa deset puta većom selektivnošću u odnosu na 5-HT2C, i bez znatnog afiniteta ili aktivnosti na 5-HT2B ili dopaminskim receptorima.[3] Ovaj lek je istraživan kao mogući tretman za Parkinsonovu psihozu,[4] i kao dodatni tretman za šizofreniju zajedno sa antipsihoticima.[5][6][7][8]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. Vanover KE, Weiner DM, Makhay M, Veinbergs I, Gardell LR, Lameh J, Del Tredici AL, Piu F, Schiffer HH, Ott TR, Burstein ES, Uldam AK, Thygesen MB, Schlienger N, Andersson CM, Son TY, Harvey SC, Powell SB, Geyer MA, Tolf BR, Brann MR, Davis RE (May 2006). "Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine2A receptor inverse agonist". J Pharmacol Exp Ther 317 (2): 910–8. PMID 16469866. doi:10.1124/jpet.105.097006. 
  4. ACADIA Pharmaceuticals. "Treating Parkinson's Disease - Clinical Trial Pimavanserin - ACADIA". http://seekingalpha.com/article/860811-acadia-a-big-move-into-parkinson-s-disease-psychosis-results. pristupljeno 11. 4. 2009.. 
  5. "ACADIA Announces Positive Results From ACP-103 Phase II Schizophrenia Co-Therapy Trial" (Press release). ACADIA Pharmaceuticals. 2007-03-19. Pristupljeno 2009-04-11. 
  6. Gardell LR, Vanover KE, Pounds L, Johnson RW, Barido R, Anderson GT, Veinbergs I, Dyssegaard A, Brunmark P, Tabatabaei A, Davis RE, Brann MR, Hacksell U, Bonhaus DW (August 2007). "ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models". J Pharmacol Exp Ther 322 (2): 862–70. PMID 17519387. doi:10.1124/jpet.107.121715. 
  7. Vanover KE, Betz AJ, Weber SM, Bibbiani F, Kielaite A, Weiner DM, Davis RE, Chase TN, Salamone JD (October 2008). "A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model". Pharmacol Biochem Behav 90 (4): 540–4. PMC 2806670. PMID 18534670. doi:10.1016/j.pbb.2008.04.010. 
  8. Abbas A, Roth BL (December 2008). "Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders". Expert Opin Pharmacother 9 (18): 3251–9. PMID 19040345. doi:10.1517/14656560802532707. 

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