Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant

  title={Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant},
  author={Hyacinth C. Akunne and Kim T. Zoski and Steven Z. Whetzel and J. J. Cordon and R. M Brandon and F Roman and Thomas A. Pugsley},

Potential antidepressant activity of sigma ligands.

  • G. Skuza
  • Biology, Psychology
    Polish journal of pharmacology
  • 2003
A potential antidepressant activity of sigma1 receptor agonists has been postulated, since the antidepressive-like actions of these compounds have been shown in animal models.

A potential antidepressant activity of SA4503, a selective sigma 1 receptor agonist.

The suggestion that SA4503 may have potential antidepressive properties is supported, as it shows a synergistic effect with imipramine and decreased the immobility time in the forced swimming test in rats.

A potential antidepressant activity of SA4503, a selective σ1 receptor agonist

The results presented in this paper support the suggestion that SA4503 may have potential antidepressive properties.

Involvement of the sigma1 receptor in the modulation of dopaminergic transmission by amantadine

It is demonstrated that aminoadamantanes behave as sigma1 receptor agonists, and an involvement of this receptor in modulating dopamine receptors exerted by therapeutically relevant concentrations of amantadine is confirmed.

Future Antidepressants

An inventory of what is and until recently was in the antidepressant pipeline of pharmaceutical companies is presented and it is argued that it is not depression itself that should be treated, but rather that its duration should be reduced by pharmacological means.

Neuropeptide and Sigma Receptors as Novel Therapeutic Targets for the Pharmacotherapy of Depression

Among the most prevalent of mental illnesses, depression is increasing in incidence in the Western world. It presents with a wide variety of symptoms that involve both the CNS and the periphery.

The antidepressant-like effect induced by the sigma1 (σ1) receptor agonist igmesine involves modulation of intracellular calcium mobilization

The σ1 receptor-mediated behavioral effect is dependent not only on rapid Ca2+ influx, as observed for a classical antidepressant, but also on intracellular Ca2+, indicating the importance of extracellular Ca 2+ influx in the initial action of each compound.

The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats.

  • G. SkuzaZ. Rogóż
  • Biology, Psychology
    Journal of physiology and pharmacology : an official journal of the Polish Physiological Society
  • 2006
The obtained results give support to the hypothesis that sigma (particularly sigma1) receptors may be one of the possible mechanisms by which drugs induce antidepressant-like activity in the forced swim test, and that this effect may be enhanced by NMDA receptor antagonists.

Neurosteroids in depression: a review

Indirect genomic and non-genomic mechanisms are involved in the neurosteroidogenic pathophysiology of depression and several findings support the hypothesis of an antidepressant effect of allopregnanolone.

Ligand : Modulation of Neuronal Activity in the Dorsal Raphe Nucleus

The current series of experiments suggest that OPC might have potential as an antidepressant with a rapid onset of action compared with selective serotonin reuptake inhibitor treatments, which initially suppress the firing activity of putative 5-HT neurons and require at least 2 to 3 weeks to restore the firingActivity to baseline neuronal firing activity through a desensitization of the 5- HT1A autoreceptor.



The Potential Contribution of Sigma Receptors to Antidepressant Actions

The search for drugs that combined the potent analgesic effect of morphine with a negligible abuse potential eventually led to the synthesis of pentazocine and cyclazocines, and it was found that the analgesic effects of these drugs were combined with dysphoric effects that were dose-related, the morphine-like effects being most pronounced at low doses and the dysphoric-hallucinogenic effects at high doses.

Current hypotheses on sigma receptors and their physiological role: possible implications in psychiatry.

  • G. Debonnel
  • Psychology, Biology
    Journal of psychiatry & neuroscience : JPN
  • 1993
Evidence suggests that sigma receptors could be involved in the pathophysiology and/or in the treatment of schizophrenia by modulating the glutamatergic inputs, by regulating directly the firing activity of dopaminergic neurons, or by both mechanisms.

Receptor adaptations to centrally acting drugs.

This review focuses on studies of eNS receptors identified by radioligand binding techniques and the influences of chronic drug treatments upon their number and affinity.

Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907.

Findings indicating that PD 128907 shows a preference for DA D3 over D2L and D4.2 receptors indicates that its action at low doses may be due to interaction with D3 receptors and at higher doses, with both D2 and D 3 receptors.