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Siramesine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Siramesine
Clinical data
ATC code
  • none
Identifiers
  • 1'-{4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl}-3H-spiro[2-benzofuran-1,4'-piperidine]
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC30H31FN2O
Molar mass454.589 g·mol−1
3D model (JSmol)
  • C1CN(CCC12C3=CC=CC=C3CO2)CCCCC4=CN(C5=CC=CC=C54)C6=CC=C(C=C6)F
  • InChI=1S/C30H31FN2O/c31-25-12-14-26(15-13-25)33-21-23(27-9-2-4-11-29(27)33)7-5-6-18-32-19-16-30(17-20-32)28-10-3-1-8-24(28)22-34-30/h1-4,8-15,21H,5-7,16-20,22H2 ☒N
  • Key:XWAONOGAGZNUSF-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Siramesine (orLu 28-179) is asigma receptoragonist, selective for theσ2 subtype.[1] Inanimal studies, siramesine has been shown to produceanxiolytic[2] andantidepressant[3] effects. It was developed by the pharmaceutical companyH Lundbeck for the treatment ofanxiety,[4] although development was discontinued after clinical trials showed a lack of efficacy inhumans. Siramesine has been shown to produce an enhanced antidepressant effect when co-administered withNMDA antagonists.[5] It has also been used to study theσ2 activity ofcocaine,[6] and has been shown to produceanticancer properties bothin vitro[7] andin vivo.[8]

References

[edit]
  1. ^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.doi:10.1016/s0028-3908(02)00071-0.PMID 12213263.S2CID 140206932.
  2. ^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.doi:10.1016/S0022-3565(24)37124-1.PMID 9400007.
  3. ^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.doi:10.1097/00008877-200004000-00003.PMID 10877116.S2CID 22007769.
  4. ^Heading C (February 2001). "Siramesine H Lundbeck".Current Opinion in Investigational Drugs.2 (2):266–70.PMID 11816842.
  5. ^Skuza G, Rogoz Z (June 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.57 (2):217–29.PMID 16845227.
  6. ^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.
  7. ^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.
  8. ^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.

External links

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σ2
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