Description
DTG (97-39-2) is an agonist of the sigma (σ) receptor1with roughly equal potency against both subtypes (σ1 and σ2 IC50’s ~ 30nM)2.
Uses
DTG is a selective ligand for the sigma-binding site. DTG has high binding affinity.
Definition
ChEBI: 1,2-bis(2-methylphenyl)guanidine is a member of toluenes.
General Description
1,3-Di-
o-tolylguanidine is a selective σ-receptor agonist. 1,3-Di-
o-tolylguanidine is σ site ligand and its interaction with dopamine drugs were studied in Wistar rats and Albino Swiss mice.
Flammability and Explosibility
Non flammable
Biological Activity
Displays high and roughly equal affinity for both σ 1 and σ 2 receptors.
Safety Profile
Poison by ingestion and
intraperitoneal routes. When heated to
decomposition it emits toxic fumes of NOx.
Purification Methods
The guanidine crystallises from aqueous EtOH. The sulfate has m 253-254o(dec, H2O). [Beilstein 12 H 803, 12 II 445, 12 III 1871, 16 IV 1764]
References
[1] E WEBER. 1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1986, 83 22: 8784-8788. DOI:
10.1073/pnas.83.22.8784[2] MICHAEL W. SCHERZ. Synthesis and structure-activity relationships of N,N’-di-o-tolylguanidine analogs, high-affinity ligands for the haloperidol-sensitive .sigma. receptor[J]. Journal of Medicinal Chemistry, 1990, 33 9: 2421-2429. DOI:
10.1021/jm00171a016
