Di-o-tolylguanidine

Description

DTG (97-39-2) is an agonist of the sigma (σ) receptor1?with roughly equal potency against both subtypes (σ1 and σ2 IC50’s ~ 30nM)2.

The Uses of Di-o-tolylguanidine

DTG is a selective ligand for the sigma-binding site. DTG has high binding affinity.

What are the applications of Application

DTG is a sigma receptor that displays a high affinity for σ1 and σ2 receptors

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) Weber?et al.?(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. USA,?83?8784 2) Scherz?et al.?(1990),?Synthesis and Structure-Activity Relationships of N,N’-Di-o-tolylguanidine Analogues, High-Affinity Ligands for the Haloperidol-Sensitive σ Receptor; J. Med. Chem.,?33?2421