Chemistry:Igmesine
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Short description: Chemical compound
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| Formula | C23H29N |
| Molar mass | 319.492 g·mol−1 |
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Igmesine (JO-1,784) is a sigma receptor agonist (IC50 = 39 nM (rat brain)).[1][2] It has neuroprotective and antidepressant-like effects in animal studies,[3][4] as well as nootropic effects in models of age-related cognitive decline.[5] 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.[2] However, in a large phase III clinical trial, igmesine failed to show significant effectiveness for depression.[6] The drug has not been developed further.[7]
References
- ↑ "JO 1784, a potent and selective ligand for rat and mouse brain sigma-sites". The Journal of Pharmacy and Pharmacology 42 (6): 439–40. June 1990. doi:10.1111/j.2042-7158.1990.tb06588.x. PMID 1979628.
- ↑ 2.0 2.1 "Sigma receptors: potential targets for a new class of antidepressant drug". Pharmacol. Ther. 127 (3): 271–82. 2010. doi:10.1016/j.pharmthera.2010.04.003. PMID 20438757.
- ↑ "The sigma receptor ligand JO 1784 (igmesine hydrochloride) is neuroprotective in the gerbil model of global cerebral ischaemia". European Journal of Pharmacology 283 (1–3): 217–25. September 1995. doi:10.1016/0014-2999(95)00356-P. PMID 7498313.
- ↑ "Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant". Neuropharmacology 41 (1): 138–49. July 2001. doi:10.1016/S0028-3908(01)00049-1. PMID 11445194.
- ↑ "Beneficial effects of sigma agonists on the age-related learning impairment in the senescence-accelerated mouse (SAM)". Brain Research 733 (2): 219–30. September 1996. doi:10.1016/0006-8993(96)00565-3. PMID 8891305.
- ↑ "Targeting ligand-operated chaperone sigma-1 receptors in the treatment of neuropsychiatric disorders". Expert Opin. Ther. Targets 15 (5): 557–77. 2011. doi:10.1517/14728222.2011.560837. PMID 21375464.
- ↑ "Clinical trials with sigma ligands". Pharmacopsychiatry 37 Suppl 3: S214–20. November 2004. doi:10.1055/s-2004-832680. PMID 15547788.
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