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Igmesine

Chemical compound

Chemical compound

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Igmesine (JO-1,784) is a sigma receptor agonist (IC50 = 39 nM (rat brain)). It has neuroprotective and antidepressant-like effects in animal studies, as well as nootropic effects in models of age-related cognitive decline. In two phase II clinical trials, igmesine was found to be effective in the treatment of depression and was as active as the comparator fluoxetine. However, in a large phase III clinical trial, igmesine failed to show significant effectiveness for depression. The drug has not been developed further.

References

References

  1. (June 1990). "JO 1784, a potent and selective ligand for rat and mouse brain sigma-sites". The Journal of Pharmacy and Pharmacology.
  2. (2010). "Sigma receptors: potential targets for a new class of antidepressant drug". Pharmacol. Ther..
  3. (September 1995). "The sigma receptor ligand JO 1784 (igmesine hydrochloride) is neuroprotective in the gerbil model of global cerebral ischaemia". European Journal of Pharmacology.
  4. (July 2001). "Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant". Neuropharmacology.
  5. (September 1996). "Beneficial effects of sigma agonists on the age-related learning impairment in the senescence-accelerated mouse (SAM)". Brain Research.
  6. (2011). "Targeting ligand-operated chaperone sigma-1 receptors in the treatment of neuropsychiatric disorders". Expert Opin. Ther. Targets.
  7. (November 2004). "Clinical trials with sigma ligands". Pharmacopsychiatry.
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amines alkene-derivatives cyclopropyl-compounds sigma-agonists
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