Ciproksifan

Ciproksifan
IUPAC ime
	ciklopropil 4-(3-(1H-imidazol-4-il)propiloksi)fenil keton
Identifikatori
CAS broj	184025-19-2
ATC kod	none
PubChem	CID 6422124
IUPHAR/BPS	1265
ChEMBL	CHEMBL14638
Hemijski podaci
Formula	C16H18N2O2
Molarna masa	270,33
	SMILES C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3; ;

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.^[1]^[2]^[3]

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.^[4] 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.^[5]^[6] On takođe pojačava dejstvo antipsihotičkih lekova, te se smatra da može da bude koristan kao komponenta tretmana šizofrenije.^[7]

Reference

^ Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). „The histamine H₃ receptor as a novel therapeutic target for cognitive and sleep disorders”. Trends Pharmacol. Sci. 25 (12): 618—25. PMID 15530639. doi:10.1016/j.tips.2004.10.003.
^ Passani MB, Giannoni P, Bucherelli C, Baldi E, Blandina P (2007). „Histamine in the brain: beyond sleep and memory”. Biochem. Pharmacol. 73 (8): 1113—22. PMID 17241615. doi:10.1016/j.bcp.2006.12.002.
^ Parmentier R, Anaclet C, Guhennec C, Brousseau E, Bricout D, Giboulot T, Bozyczko-Coyne D, Spiegel K, Ohtsu H, Williams M, Lin JS (2007). „The brain H₃-receptor as a novel therapeutic target for vigilance and sleep-wake disorders”. Biochem. Pharmacol. 73 (8): 1157—71. PMID 17288995. doi:10.1016/j.bcp.2007.01.002.
^ Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H (2008). „Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H₃ receptor antagonists”. J. Pharmacol. Exp. Ther. 325 (3): 902—9. PMID 18305012. doi:10.1124/jpet.107.135343.
^ LLigneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J (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 (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. PMID 15251226. doi:10.1016/j.pharmthera.2004.05.001.
^ Pillot C, Ortiz J, Héron A, Ridray S, Schwartz JC, Arrang JM (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

[pmid15530639-1] Passani MB, Lin JS, Hancock A, Crochet S, Blandina P (2004). „The histamine H₃ receptor as a novel therapeutic target for cognitive and sleep disorders”. Trends Pharmacol. Sci. 25 (12): 618—25. PMID 15530639. doi:10.1016/j.tips.2004.10.003.

[pmid17241615-2] Passani MB, Giannoni P, Bucherelli C, Baldi E, Blandina P (2007). „Histamine in the brain: beyond sleep and memory”. Biochem. Pharmacol. 73 (8): 1113—22. PMID 17241615. doi:10.1016/j.bcp.2006.12.002.

[pmid17288995-3] Parmentier R, Anaclet C, Guhennec C, Brousseau E, Bricout D, Giboulot T, Bozyczko-Coyne D, Spiegel K, Ohtsu H, Williams M, Lin JS (2007). „The brain H₃-receptor as a novel therapeutic target for vigilance and sleep-wake disorders”. Biochem. Pharmacol. 73 (8): 1157—71. PMID 17288995. doi:10.1016/j.bcp.2007.01.002.

[pmid18305012-4] Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H (2008). „Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H₃ receptor antagonists”. J. Pharmacol. Exp. Ther. 325 (3): 902—9. PMID 18305012. doi:10.1124/jpet.107.135343.

[pmid9808693-5] LLigneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J (1998). „Neurochemical and behavioral effects of ciproxifan, a potent histamine H₃-receptor antagonist”. J. Pharmacol. Exp. Ther. 287 (2): 658—66. PMID 9808693.

[pmid15251226-6] Witkin JM, Nelson DL (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. PMID 15251226. doi:10.1016/j.pharmthera.2004.05.001.

[pmid12177222-7] Pillot C, Ortiz J, Héron A, Ridray S, Schwartz JC, Arrang JM (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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