Ditolylguanidine (DTG) is a sigma receptor agonist. It is somewhat selective for sigma receptors, but non-selective between the two sigma receptor subtypes, binding to both σ₁ and σ₂ with equal affinity. It has neuroprotective and antidepressant effects, and potentiates the effects of NMDA antagonists.

N,N′-Di-o-tolylguanidine is a flammable, white solid that is practically insoluble in water. It decomposes upon heating, potentially releasing nitrogen oxides, carbon monoxide, and carbon dioxide.

N,N′-Di-o-tolylguanidine is not itself carcinogenic, but due to the manufacturing process, it may still contain o-toluidine, which is carcinogenic. Therefore, if the o-toluidine content exceeds 0.1 percent, the mixture should be considered carcinogenic.