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]
^Glennon RA (October 2005). "Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach". Mini Reviews in Medicinal Chemistry. 5 (10): 927–940.
doi:
10.2174/138955705774329519.
PMID16250835.
^Katnik C, Guerrero WR, Pennypacker KR, Herrera Y, Cuevas J (December 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): 1355–1365.
doi:
10.1124/jpet.106.107557.
PMID16988055.
S2CID14582181.
^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): 1149–1152.
PMID14730114.
^Monnet FP, Morin-Surun MP, Leger J, Combettes L (November 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): 705–712.
doi:
10.1124/jpet.103.053447.
PMID12975497.
S2CID35397107.