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Siramesin
IUPAC ime
	1'4-[1-(4-fluorophenyl)-1H-indol-3-yl]butyl3H-spiro[2-benzofuran-1,4'-piperidine]
Identifikatori
CAS broj	147817-50-3
ATC kod	none
PubChem	CID 9829526
Hemijski podaci
Formula	C30H31FN2O
Molarna masa	454.59 g/mol
	SMILES C1CN(CCC12C3=CC=CC=C3CO2)CCCCC4=CN(C5=CC=CC=C54)C6=CC=C(C=C6)F; ;

Siramesin (Lu 28-179) je agonist sigma receptora. On je selektivan za σ2 tip.^[1]

U istraživanjima na životinjama, za siramesin je utvrđeno da proizvodi anksiolitičke^[2] i antidepresivne^[3] efekte. Njega je razvila farmaceutska kompanija H Lundbek za lečenje anksioznosti.^[4] Razvoj je prekinut nakon što su klinička ispitivanja pokazala da nema dovoljnu efikasnost kod čoveka.

Za siramesin je pokazano da proizvodi povećane antidepresivne efekte kad se dozira zajedno sa NMDA antagonistima.^[5] On je takođe bio korišten u studijama σ2 aktivnosti kokaina^[6], a i bilo je pokazano da ima antikancerogene osobine in vitro^[7] i in vivo.^[8]

Reference

^ Søby KK, Mikkelsen JD, Meier E, Thomsen C (2002). „Lu 28-179 labels a sigma(2)-site in rat and human brain”. Neuropharmacology. 43 (1): 95—100. PMID 12213263. doi:10.1016/s0028-3908(02)00071-0. Приступљено 26. 04. 2011.
^ Sánchez C, Arnt J, Costall B, Kelly ME, Meier E, Naylor RJ, Perregaard J (1997). „The selective sigma2-ligand Lu 28-179 has potent anxiolytic-like effects in rodents”. The Journal of Pharmacology and Experimental Therapeutics. 283 (3): 1323—32. PMID 9400007.
^ Sánchez C, Papp M (2000). „The selective sigma2 ligand Lu 28-179 has an antidepressant-like profile in the rat chronic mild stress model of depression”. Behavioural Pharmacology. 11 (2): 117—24. PMID 10877116. doi:10.1097/00008877-200004000-00003. Приступљено 26. 04. 2011. ^{[мртва веза]}
^ Heading C. Siramesine H Lundbeck. Heading, C. (фебруар 2001). „Siramesine H Lundbeck”. Current Opinion in Investigational Drugs. 2 (2): 266—70. PMID 11816842. .
^ Skuza G, Rogóz Z (2006). „The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats” (PDF). Journal of Physiology and Pharmacology : An Official Journal of the Polish Physiological Society. 57 (2): 217—29. PMID 16845227. Приступљено 26. 04. 2011.
^ Nuwayhid SJ, Werling LL (2006). „Sigma2 (sigma2) receptors as a target for cocaine action in the rat striatum”. European Journal of Pharmacology. 535 (1–3): 98—103. PMID 16480713. doi:10.1016/j.ejphar.2005.12.077. Приступљено 26. 04. 2011.
^ Ostenfeld MS, Fehrenbacher N, Høyer-Hansen M, Thomsen C, Farkas T, Jäättelä M (2005). „Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress”. Cancer Research. 65 (19): 8975—83. PMID 16204071. doi:10.1158/0008-5472.CAN-05-0269. Приступљено 26. 04. 2011.
^ Groth-Pedersen L, Ostenfeld MS, Høyer-Hansen M, Nylandsted J, Jäättelä M (2007). „Vincristine induces dramatic lysosomal changes and sensitizes cancer cells to lysosome-destabilizing siramesine”. Cancer Research. 67 (5): 2217—25. PMID 17332352. doi:10.1158/0008-5472.CAN-06-3520. Приступљено 26. 04. 2011.

Spoljašnje veze

Siramesine на US National Library of Medicine Medical Subject Headings (MeSH)

[pmid12213263-1] Søby KK, Mikkelsen JD, Meier E, Thomsen C (2002). „Lu 28-179 labels a sigma(2)-site in rat and human brain”. Neuropharmacology. 43 (1): 95—100. PMID 12213263. doi:10.1016/s0028-3908(02)00071-0. Приступљено 26. 04. 2011.

[pmid9400007-2] Sánchez C, Arnt J, Costall B, Kelly ME, Meier E, Naylor RJ, Perregaard J (1997). „The selective sigma2-ligand Lu 28-179 has potent anxiolytic-like effects in rodents”. The Journal of Pharmacology and Experimental Therapeutics. 283 (3): 1323—32. PMID 9400007.

[pmid10877116-3] Sánchez C, Papp M (2000). „The selective sigma2 ligand Lu 28-179 has an antidepressant-like profile in the rat chronic mild stress model of depression”. Behavioural Pharmacology. 11 (2): 117—24. PMID 10877116. doi:10.1097/00008877-200004000-00003. Приступљено 26. 04. 2011. ^{[мртва веза]}

[4] Heading C. Siramesine H Lundbeck. Heading, C. (фебруар 2001). „Siramesine H Lundbeck”. Current Opinion in Investigational Drugs. 2 (2): 266—70. PMID 11816842. .

[pmid16845227-5] Skuza G, Rogóz Z (2006). „The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats” (PDF). Journal of Physiology and Pharmacology : An Official Journal of the Polish Physiological Society. 57 (2): 217—29. PMID 16845227. Приступљено 26. 04. 2011.

[pmid16480713-6] Nuwayhid SJ, Werling LL (2006). „Sigma2 (sigma2) receptors as a target for cocaine action in the rat striatum”. European Journal of Pharmacology. 535 (1–3): 98—103. PMID 16480713. doi:10.1016/j.ejphar.2005.12.077. Приступљено 26. 04. 2011.

[pmid16204071-7] Ostenfeld MS, Fehrenbacher N, Høyer-Hansen M, Thomsen C, Farkas T, Jäättelä M (2005). „Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress”. Cancer Research. 65 (19): 8975—83. PMID 16204071. doi:10.1158/0008-5472.CAN-05-0269. Приступљено 26. 04. 2011.

[pmid17332352-8] Groth-Pedersen L, Ostenfeld MS, Høyer-Hansen M, Nylandsted J, Jäättelä M (2007). „Vincristine induces dramatic lysosomal changes and sensitizes cancer cells to lysosome-destabilizing siramesine”. Cancer Research. 67 (5): 2217—25. PMID 17332352. doi:10.1158/0008-5472.CAN-06-3520. Приступљено 26. 04. 2011.

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