Pimavanserin

Pimavanserin
IUPAC ime
	N-(4-fluorofenilmetil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloksi)fenilmetil)karbamid
Klinički podaci
Način primene	Oralno
Identifikatori
CAS broj	706779-91-1 ; 706782-28-7 (tartarat)
ATC kod	none
PubChem	CID 10071196
UNII	JZ963P0DIK
Hemijski podaci
Formula	C25H34FN3O2
Molarna masa	427,553 g/mol
	SMILES CC(C)COc3ccc(cc3)CNC(=O)N(C(CC2)CCN2C)Cc(cc1)ccc1F; ;

Pimavanserin (ACP-103) je lek koji deluje kao inverzni agonist na serotoninskom receptoru 5-HT_2A, sa deset puta većom selektivnošću u odnosu na 5-HT_2C, i bez znatnog afiniteta ili aktivnosti na 5-HT_2B ili dopaminskim receptorima.^[1] Ovaj lek je istraživan kao mogući tretman za Parkinsonovu psihozu,^[2] i kao dodatni tretman za šizofreniju zajedno sa antipsihoticima.^[3]^[4]^[5]^[6]

Reference уреди

^ 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 (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-hydroxytryptamine_2A receptor inverse agonist”. J Pharmacol Exp Ther. 317 (2): 910—8. PMID 16469866. doi:10.1124/jpet.105.097006.
^ ACADIA Pharmaceuticals. „Treating Parkinson's Disease - Clinical Trial Pimavanserin - ACADIA”. Приступљено 11. 4. 2009.
^ „ACADIA Announces Positive Results From ACP-103 Phase II Schizophrenia Co-Therapy Trial” (Саопштење). ACADIA Pharmaceuticals. 19. 3. 2007. Приступљено 11. 4. 2009. ^{[мртва веза]}
^ 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 (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.
^ Vanover KE, Betz AJ, Weber SM, Bibbiani F, Kielaite A, Weiner DM, Davis RE, Chase TN, Salamone JD (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.
^ Abbas A, Roth BL (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.

Spoljašnje veze уреди

[pmid16469866-1] 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 (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-hydroxytryptamine_2A receptor inverse agonist”. J Pharmacol Exp Ther. 317 (2): 910—8. PMID 16469866. doi:10.1124/jpet.105.097006.

[urlTreating_Parkinsons_Disease_-_Clinical_Trial_Pimavanserin_-_ACADIA-2] ACADIA Pharmaceuticals. „Treating Parkinson's Disease - Clinical Trial Pimavanserin - ACADIA”. Приступљено 11. 4. 2009.

[pressReleaseSchiz-3] „ACADIA Announces Positive Results From ACP-103 Phase II Schizophrenia Co-Therapy Trial” (Саопштење). ACADIA Pharmaceuticals. 19. 3. 2007. Приступљено 11. 4. 2009. ^{[мртва веза]}

[pmid17519387-4] 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 (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.

[pmid18534670-5] Vanover KE, Betz AJ, Weber SM, Bibbiani F, Kielaite A, Weiner DM, Davis RE, Chase TN, Salamone JD (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.

[pmid19040345-6] Abbas A, Roth BL (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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