Ditolilgvanidin

Ditolilgvanidin
IUPAC ime
1,2-bis(2-methylphenyl)guanidine
Identifikatori
CAS broj97-39-2 ДаY
ATC kodnone
PubChemCID 7333
ChemSpider7056 ДаY
ChEMBLCHEMBL282433 ДаY
Hemijski podaci
FormulaC15H17N3
Molarna masa239.316 g/mol
  • N(=C(/Nc1ccccc1C)N)\c2ccccc2C
  • InChI=1S/C15H17N3/c1-11-7-3-5-9-13(11)17-15(16)18-14-10-6-4-8-12(14)2/h3-10H,1-2H3,(H3,16,17,18) ДаY
  • Key:OPNUROKCUBTKLF-UHFFFAOYSA-N ДаY

Ditolilgvanidin je agonist sigma receptora.[1] On je selektivan za sigma receptore, ali nije selektivan između dva tipa sigma receptora, već se vezuje sa jednakim afinitetom za σ1 i σ2 .[2] On ima neuroprotektivne[3] i antidepresivne efekte,[4] i pojačava dejstvo NMDA antagonista.[5]

  1. ^ Weber E, Sonders M, Quarum M, McLean S, Pou S, Keana JF (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. PMC 387016Слободан приступ. PMID 2877462. doi:10.1073/pnas.83.22.8784. 
  2. ^ 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. 
  3. ^ 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. PMID 16988055. doi:10.1124/jpet.106.107557. 
  4. ^ 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. 
  5. ^ 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. PMID 12975497. doi:10.1124/jpet.103.053447. 


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