Ditolilgvanidin

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Ditolilgvanidin
(IUPAC) ime
1,2-bis(2-methylphenyl)guanidine
Klinički podaci
Identifikatori
CAS broj 97-39-2
ATC kod nije dodeljen
PubChem[1][2] 7333
ChemSpider[3] 7056
ChEMBL[4] CHEMBL282433 DaY
Hemijski podaci
Formula C15H17N3 
Mol. masa 239.316 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Ditolilgvanidin je agonist sigma receptora.[5] On je selektivan za sigma receptore, ali nije selektivan između dva tipa sigma receptora, već se vezuje sa jednakim afinitetom za σ1 i σ2 .[6] On ima neuroprotektivne[7] i antidepresivne efekte,[8] i pojačava dejstvo NMDA antagonista.[9]

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Literatura[uredi | uredi kod]

  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. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. 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
  5. Weber E, Sonders M, Quarum M, McLean S, Pou S, Keana JF (November 1986). „1,3-Di(2-(5-3H)tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs”. Proc. Natl. Acad. Sci. U.S.A. 83 (22): 8784–8. DOI:10.1073/pnas.83.22.8784. PMC 387016. PMID 2877462. 
  6. Glennon, RA (2005). „Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach.”. Mini reviews in medicinal chemistry 5 (10): 927–40. PMID 16250835. 
  7. Katnik, C; Guerrero, WR; Pennypacker, KR; Herrera, Y; Cuevas, J (2006). „Sigma-1 receptor activation prevents intracellular calcium dysregulation in cortical neurons during in vitro ischemia.”. The Journal of pharmacology and experimental therapeutics 319 (3): 1355–65. DOI:10.1124/jpet.106.107557. PMID 16988055. 
  8. Skuza, G; Rogóz, Z (2003). „Sigma1 receptor antagonists attenuate antidepressant-like effect induced by co-administration of 1,3 di-o-tolylguanidine (DTG) and memantine in the forced swimming test in rats.”. Polish journal of pharmacology 55 (6): 1149–52. PMID 14730114. 
  9. Monnet, FP; Morin-Surun, MP; Leger, J; Combettes, L (2003). „Protein kinase C-dependent potentiation of intracellular calcium influx by sigma1 receptor agonists in rat hippocampal neurons.”. The Journal of pharmacology and experimental therapeutics 307 (2): 705–12. DOI:10.1124/jpet.103.053447. PMID 12975497. 

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