Ciproksifan

Ciproksifan
(IUPAC) ime
	ciklopropil 4-(3-(1H-imidazol-4-il)propiloksi)fenil keton
Klinički podaci
Identifikatori
CAS broj	184025-19-2
ATC kod	nije dodeljen
PubChem	6422124
ChEMBL	CHEMBL14638
Hemijski podaci
Formula	C16H18N2O2
Mol. masa	270,33
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18); Key: ACQBHJXEAYTHCY-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Ciproksifan je veoma potentan histaminski H₃ inverzni agonist/antagonist.

Histaminski H₃ receptor je inhibitorni autoreceptor lociran na histaminergičkim nervnim terminalima, i učestvuje u modulaciji otpuštanja histamina u mozgu. Histamin ima pobuđivačko dejstvo na mozak putem H₁ receptora u moždanoj kori, tako da lekovi poput ciproksifana koji blokiraju H₃ receptor i konsekventno omogućavaju više histamina da bude otpušteno povećavaju budnost.^[4]^[5]^[6]

Ciproksifan proizvodi budnost i predustretljivost u životinjskim studijama, posledica čega je poboljšana spoznaja bez znatnih stimulacionih efekata pri niskim nivoima zauzeća receptora, i naglašena budnost na višim dozama.^[7] Predloženo je da on može da služi kao potencijalni tretman za poremećaje spavanja, kao što su narkolepsija, i za poboljšanje pažnje kod starih osoba, posebno pri tretiranju oboljenje kao što je Alchajmerova bolest.^[8]^[9] On takođe pojačava dejstvo antipsihotičkih lekova, te se smatra da može da bude koristan kao komponenta tretmana šizofrenije.^[10]

Reference

↑ 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
↑ 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.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (December 2004). „The histamine H₃ receptor as a novel therapeutic target for cognitive and sleep disorders”. Trends Pharmacol. Sci. 25 (12): 618–25. DOI:10.1016/j.tips.2004.10.003. PMID 15530639.
↑ Passani MB, Giannoni P, Bucherelli C, Baldi E, Blandina P (April 2007). „Histamine in the brain: beyond sleep and memory”. Biochem. Pharmacol. 73 (8): 1113–22. DOI:10.1016/j.bcp.2006.12.002. PMID 17241615.
↑ Parmentier R, Anaclet C, Guhennec C, Brousseau E, Bricout D, Giboulot T, Bozyczko-Coyne D, Spiegel K, Ohtsu H, Williams M, Lin JS (April 2007). „The brain H₃-receptor as a novel therapeutic target for vigilance and sleep-wake disorders”. Biochem. Pharmacol. 73 (8): 1157–71. DOI:10.1016/j.bcp.2007.01.002. PMID 17288995.
↑ Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H (June 2008). „Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H₃ receptor antagonists”. J. Pharmacol. Exp. Ther. 325 (3): 902–9. DOI:10.1124/jpet.107.135343. PMID 18305012.
↑ LLigneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J (November 1998). „Neurochemical and behavioral effects of ciproxifan, a potent histamine H₃-receptor antagonist”. J. Pharmacol. Exp. Ther. 287 (2): 658–66. PMID 9808693.
↑ Witkin JM, Nelson DL (July 2004). „Selective histamine H₃ receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous system”. Pharmacol. Ther. 103 (1): 1–20. DOI:10.1016/j.pharmthera.2004.05.001. PMID 15251226.
↑ Pillot C, Ortiz J, Héron A, Ridray S, Schwartz JC, Arrang JM (August 2002). „Ciproxifan, a histamine H₃-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat”. J. Neurosci. 22 (16): 7272–80. PMID 12177222.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[pmid15530639-4] Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (December 2004). „The histamine H₃ receptor as a novel therapeutic target for cognitive and sleep disorders”. Trends Pharmacol. Sci. 25 (12): 618–25. DOI:10.1016/j.tips.2004.10.003. PMID 15530639.

[pmid17241615-5] Passani MB, Giannoni P, Bucherelli C, Baldi E, Blandina P (April 2007). „Histamine in the brain: beyond sleep and memory”. Biochem. Pharmacol. 73 (8): 1113–22. DOI:10.1016/j.bcp.2006.12.002. PMID 17241615.

[pmid17288995-6] Parmentier R, Anaclet C, Guhennec C, Brousseau E, Bricout D, Giboulot T, Bozyczko-Coyne D, Spiegel K, Ohtsu H, Williams M, Lin JS (April 2007). „The brain H₃-receptor as a novel therapeutic target for vigilance and sleep-wake disorders”. Biochem. Pharmacol. 73 (8): 1157–71. DOI:10.1016/j.bcp.2007.01.002. PMID 17288995.

[pmid18305012-7] Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H (June 2008). „Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H₃ receptor antagonists”. J. Pharmacol. Exp. Ther. 325 (3): 902–9. DOI:10.1124/jpet.107.135343. PMID 18305012.

[pmid9808693-8] LLigneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J (November 1998). „Neurochemical and behavioral effects of ciproxifan, a potent histamine H₃-receptor antagonist”. J. Pharmacol. Exp. Ther. 287 (2): 658–66. PMID 9808693.

[pmid15251226-9] Witkin JM, Nelson DL (July 2004). „Selective histamine H₃ receptor antagonists for treatment of cognitive deficiencies and other disorders of the central nervous system”. Pharmacol. Ther. 103 (1): 1–20. DOI:10.1016/j.pharmthera.2004.05.001. PMID 15251226.

[pmid12177222-10] Pillot C, Ortiz J, Héron A, Ridray S, Schwartz JC, Arrang JM (August 2002). „Ciproxifan, a histamine H₃-receptor antagonist/inverse agonist, potentiates neurochemical and behavioral effects of haloperidol in the rat”. J. Neurosci. 22 (16): 7272–80. PMID 12177222.

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