Ditolylguanidine Explained

Ditolylguanidine is a sigma receptor agonist.[1] It is somewhat[2] selective for sigma receptors, but non-selective between the two sigma receptor subtypes, binding to both σ1 and σ2 with equal affinity.[3] It has neuroprotective[4] and antidepressant effects,[5] and potentiates the effects of NMDA antagonists.[6]

See also

Notes and References

  1. Weber E, Sonders M, Quarum M, McLean S, Pou S, Keana JF . 1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs . Proceedings of the National Academy of Sciences of the United States of America . 83 . 22 . 8784–8788 . November 1986 . 2877462 . 387016 . 10.1073/pnas.83.22.8784 . 1986PNAS...83.8784W . free .
  2. Web site: 1,3-Di-o-tolylguanidine C15H17N3 . PubChem . U.S. National Library of Medicine . en. 2017-06-07. 2021-01-08. https://web.archive.org/web/20210108060333/https://pubchem.ncbi.nlm.nih.gov/compound/7333#section=BioAssay-Results. live.
  3. Glennon RA . Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach . Mini Reviews in Medicinal Chemistry . 5 . 10 . 927–940 . October 2005 . 16250835 . 10.2174/138955705774329519 .
  4. Katnik C, Guerrero WR, Pennypacker KR, Herrera Y, Cuevas J . Sigma-1 receptor activation prevents intracellular calcium dysregulation in cortical neurons during in vitro ischemia . The Journal of Pharmacology and Experimental Therapeutics . 319 . 3 . 1355–1365 . December 2006 . 16988055 . 10.1124/jpet.106.107557 . 14582181 .
  5. Skuza G, Rogóz Z . 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 . 1149–1152 . 2003 . 14730114 .
  6. Monnet FP, Morin-Surun MP, Leger J, Combettes L . 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 . 705–712 . November 2003 . 12975497 . 10.1124/jpet.103.053447 . 35397107 .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Ditolylguanidine".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.