Biomaterial Database

Effect of 1,3-di-o-tolylguanidine (DTG), rimcazole and EMD 57445, the sigma receptor ligands, in the forced swimming test. 1997

G Skuza, and Z Rogóz

Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.

As it is known, sigma receptor ligands have been able to modulate the central neurotransmitter systems, including noradrenergic-, NMDA-ergic- and dopaminergic ones, which are essential for the mechanism of action of antidepressant drugs. Therefore, it can be assumed that some selective sigma ligands can possess antidepressant-like activity. In the present studies 1,3-di-o-tolylguanidine (DTG), rimcazole (RIM) and EMD 57445 were examined in the forced swimming test in rats and mice. DTG and RIM decreased the immobility time in mice. EMD 57445 was inactive but it antagonized the anti-immobility effects of DTG and RIM. Both latter drugs did not change the locomotor activity of mice, EMD 57445 at higher dose decreased it. In addition, DTG showed antidepressant-like activity in rats, this effect being counteracted by EMD 57445. At the same time both drugs attenuated the spontaneous motor activity in rats. Taken together, the present results suggested that DTG and RIM may possess sigma agonistic activity while EMD 57445--the antagonistic one. Further investigations are needed to support agonistic/antagonistic activities of the studied sigma ligands and to elucidate the potential involvement of sigma site subtypes in this model.

UI	MeSH Term	Description	Entries
D007103	Immobilization	The restriction of the MOVEMENT of whole or part of the body by physical means (RESTRAINT, PHYSICAL) or chemically by ANALGESIA, or the use of TRANQUILIZING AGENTS or NEUROMUSCULAR NONDEPOLARIZING AGENTS. It includes experimental protocols used to evaluate the physiologic effects of immobility.	Hypokinesia, Experimental,Experimental Hypokinesia,Experimental Hypokinesias,Hypokinesias, Experimental
D008024	Ligands	A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)	Ligand
D008297	Male		Males
D009043	Motor Activity	Body movements of a human or an animal as a behavioral phenomenon.	Activities, Motor,Activity, Motor,Motor Activities
D010080	Oxazoles	Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.	Oxazole,1,3-Oxazolium-5-Oxides,Munchnones,1,3 Oxazolium 5 Oxides
D010880	Piperidines	A family of hexahydropyridines.
D002227	Carbazoles	Benzo-indoles similar to CARBOLINES which are pyrido-indoles. In plants, carbazoles are derived from indole and form some of the INDOLE ALKALOIDS.
D006146	Guanidines	A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000928	Antidepressive Agents	Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems.	Antidepressant,Antidepressant Drug,Antidepressant Medication,Antidepressants,Antidepressive Agent,Thymoanaleptic,Thymoanaleptics,Thymoleptic,Thymoleptics,Antidepressant Drugs,Agent, Antidepressive,Drug, Antidepressant,Medication, Antidepressant