1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.

“…Prior to then, many investigators confirmed the ability of select antidepressant drugs, including selective serotonin reuptake inhibitors (SSRIs), monoamine oxidase inhibitors, and tricyclic antidepressants (TCAs), to interact with σ receptors (Schmidt et al, 1989;Itzhak and Kassim, 1990;Weber et al, 1986).…”

Section: Introductionmentioning

confidence: 99%

Novel sigma (σ) receptor agonists produce antidepressant-like effects in mice

Wang

Mack

Coop

et al. 2007

European Neuropsychopharmacology

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Many antidepressant drugs interact with σ receptors and accumulating evidence suggests that these proteins mediate antidepressant-like effects in animals and humans. σ Receptors are localized in brain regions affected in depression, further strengthening the hypothesis that they represent logical drug development targets. In this study, two novel σ receptor agonists (UMB23, UMB82) were evaluated for antidepressant-like activity in mice. First, radioligand binding studies confirmed that the novel compounds had preferential affinity for σ receptors. Second, the forced swim test, a well established animal model for screening potential antidepressant drugs, showed that both compounds dose-dependently reduced immobility time. The σ receptor antagonist BD1047 attenuated the antidepressant-like effects of UMB23 and UMB82. Third, locomotor activity suggested that the effects of UMB23 and UMB82 in the forced swim test were not due to non-specific motor activating effects. Together, the data provide further evidence that σ receptor agonists represent a possible new class of antidepressant medication.

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“…The rats were administered with one dose diary during 27 days, either of the sigma agonist 1,3-di-o-tolyl-guanidine (DTG; Tocris Biosciences) 10 mg/kg (i.p. ), [50] or phosphate buffer saline (vehicle).…”

Section: Drug Administrationmentioning

confidence: 99%

Differential Effect on Two Immobility Responses by Chronic Administration of 1,3-di-o-Tolyl-Guanidine (Sigma Receptor Agonist) in Rats with Neonatal Ventral Hippocampal Lesion

Jaramillo¹,

Cruz²,

Vargas³

et al. 2014

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The effect of chronic administration of the sigma agonist: 1,3-di-o-tolyl-guanidine (DTG), in neonatal ventral hippocampal lesioned (nVHL) rats, on the immobility by clamping and dorsal immobility, were investigated. The nVHL increases the duration of immobility by clamping, but does not affect the duration of the dorsal immobility. We found that DTG augments the duration of the dorsal immobility in the unlesioned rats, but does not modify the duration of immobility induced by clamping the neck. DTG also counteracts the increase in the duration of the immobility by clamping produced by nVHL. However, the increase in the duration of the dorsal immobility produced by DTG is counteracted by nVHL. These results are discussed with respect to the differential effect on the two immobility responses tested, suggesting that they are different forms of immobility mediated by different mechanisms although they behaviorally share common characteristics.

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1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.

Cited by 286 publications

References 25 publications

Synthesis and evaluation of optically pure [³H]‐(+)‐pentazocine, a highly potent and selective radioligand for σ receptors

Synthesis and evaluation of optically pure [³H]‐(+)‐pentazocine, a highly potent and selective radioligand for σ receptors

Novel sigma (σ) receptor agonists produce antidepressant-like effects in mice

Differential Effect on Two Immobility Responses by Chronic Administration of 1,3-di-o-Tolyl-Guanidine (Sigma Receptor Agonist) in Rats with Neonatal Ventral Hippocampal Lesion

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1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs.

Cited by 286 publications

References 25 publications

Synthesis and evaluation of optically pure [3H]‐(+)‐pentazocine, a highly potent and selective radioligand for σ receptors

Synthesis and evaluation of optically pure [3H]‐(+)‐pentazocine, a highly potent and selective radioligand for σ receptors

Novel sigma (σ) receptor agonists produce antidepressant-like effects in mice

Differential Effect on Two Immobility Responses by Chronic Administration of 1,3-di-o-Tolyl-Guanidine (Sigma Receptor Agonist) in Rats with Neonatal Ventral Hippocampal Lesion

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Synthesis and evaluation of optically pure [³H]‐(+)‐pentazocine, a highly potent and selective radioligand for σ receptors

Synthesis and evaluation of optically pure [³H]‐(+)‐pentazocine, a highly potent and selective radioligand for σ receptors