Siramesin

Siramesin
(IUPAC) ime
1'4-[1-(4-fluorophenyl)-1H-indol-3-yl]butyl3H-spiro[2-benzofuran-1,4'-piperidine]
Klinički podaci
Identifikatori
CAS broj 147817-50-3
ATC kod nije dodeljen
PubChem[1][2] 9829526
Hemijski podaci
Formula C30H31FN2O 
Mol. masa 454.59 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Siramesin (Lu 28-179) je agonist sigma receptora. On je selektivan za σ2 tip.[3]

U istraživanjima na životinjama, za siramesin je utvrđeno da proizvodi anksiolitičke[4] i antidepresivne[5] efekte. Njega je razvila farmaceutska kompanija H Lundbek za lečenje anksioznosti.[6] 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.[7] On je takođe bio korišten u studijama σ2 aktivnosti kokaina[8], a i bilo je pokazano da ima antikancerogene osobine in vitro[9] i in vivo.[10]

Reference

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  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. ↑ Søby KK, Mikkelsen JD, Meier E, Thomsen C (July 2002). „Lu 28-179 labels a sigma(2)-site in rat and human brain”. Neuropharmacology 43 (1): 95–100. PMID 12213263. Pristupljeno 2011-04-26. 
  4. ↑ Sánchez C, Arnt J, Costall B, Kelly ME, Meier E, Naylor RJ, Perregaard J (December 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. Pristupljeno 2011-04-26. [mrtav link]
  5. ↑ Sánchez C, Papp M (April 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. Pristupljeno 2011-04-26. 
  6. ↑ Heading C. Siramesine H Lundbeck. Current Opinion in Investigational Drugs. 2001 Feb;2(2):266-70.
  7. ↑ Skuza G, Rogóz Z (June 2006). „The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats”. Journal of Physiology and Pharmacology : an Official Journal of the Polish Physiological Society 57 (2): 217–29. PMID 16845227. Pristupljeno 2011-04-26. 
  8. ↑ Nuwayhid SJ, Werling LL (March 2006). „Sigma2 (sigma2) receptors as a target for cocaine action in the rat striatum”. European Journal of Pharmacology 535 (1-3): 98–103. DOI:10.1016/j.ejphar.2005.12.077. PMID 16480713. Pristupljeno 2011-04-26. 
  9. ↑ Ostenfeld MS, Fehrenbacher N, Høyer-Hansen M, Thomsen C, Farkas T, Jäättelä M (October 2005). „Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress”. Cancer Research 65 (19): 8975–83. DOI:10.1158/0008-5472.CAN-05-0269. PMID 16204071. Pristupljeno 2011-04-26. 
  10. ↑ Groth-Pedersen L, Ostenfeld MS, Høyer-Hansen M, Nylandsted J, Jäättelä M (March 2007). „Vincristine induces dramatic lysosomal changes and sensitizes cancer cells to lysosome-destabilizing siramesine”. Cancer Research 67 (5): 2217–25. DOI:10.1158/0008-5472.CAN-06-3520. PMID 17332352. Pristupljeno 2011-04-26. 

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