Edonerpic maleate (T-817 maleate) (Synonyms: T-187MA) |
| Catalog No.GC30823 |
Edonerpic maleate (T-817 maleate) is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).
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Cas No.: 519187-97-4
Sample solution is provided at 25 µL, 10mM.
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T-817MA [1-{3-[2-(1-Benzothiophen-5-yl)ethoxy] propyl}-3-azetidinol maleate] is a newly synthesized agent for Alzheimer's disease (AD) treatment with neuroprotective effects against toxicity from amyloid-β peptide (Aβ) and actions promoting neurite outgrowth[1].
T-817MA was pretreated for 24 h,T-817MA significantly prevented neuronal damage caused by H2O2 treatment at 0.1 and 1 uM[1]. T-817MA at 0.1 and 1microM attenuated the neurotoxicity in a dose-dependent way and the protective effect required pretreatment for more than 8h. T-817MA attenuated SNP-induced decrease in mitochondrial transmembrane potential[5].
T-817MA (8.4 mg/kg/day; p.o.) hippocampal neurogenesis was significantly increased and spatial learning disabilities were improved in rats treated with aβ[2]. T-817MA (10 or 20 mg/kg) or vehicle was administered for 14 days. Administration of T-817MA at 20 mg/kg ameliorated Prepulse inhibition (PPI) deficits and completely reversed the decrease in the number of PV-positive GABAergic neurons in rats given MK-801[3]. T-817MA (0.21 or 0.07 mg/ml, p.o.) is effective in ameliorating sensorimotor gating deficits caused by chronic PCP treatment, possibly via neuroprotective actions[4]. T-817MA prevented the progression of motor deficit and the loss of spinal cord motor neurons in P301L mice[6]. Sustained oral administration of T-817MA significantly reduced the extent of auditory threshold shifts and outer hair cell loss, indicating that T-817MA attenuates the intense pressure-induced cochlear damage that accompanies inner ear barotrauma via antioxidative activity[7].
References:
[1]. Hirata K, Yamaguchi H, et,al.A novel neurotrophic agent, T-817MA [1-{3-[2-(1-benzothiophen-5-yl) ethoxy] propyl}-3-azetidinol maleate], attenuates amyloid-beta-induced neurotoxicity and promotes neurite outgrowth in rat cultured central nervous system neurons. J Pharmacol Exp Ther. 2005 Jul;314(1):252-9. doi: 10.1124/jpet.105.083543. Epub 2005 Mar 29. PMID: 15798005.
[2]. Kimura T, Hong Nguyen PT, et,al.T-817MA, a neurotrophic agent, ameliorates the deficits in adult neurogenesis and spatial memory in rats infused i.c.v. with amyloid-beta peptide. Br J Pharmacol. 2009 Jun;157(3):451-63. doi: 10.1111/j.1476-5381.2009.00141.x. Epub 2009 Apr 3. PMID: 19371351; PMCID: PMC2707991.
[3]. Uehara T, Sumiyoshi T, et,al. T-817MA, a novel neurotrophic agent, ameliorates loss of GABAergic parvalbumin-positive neurons and sensorimotor gating deficits in rats transiently exposed to MK-801 in the neonatal period. J Psychiatr Res. 2012 May;46(5):622-9. doi: 10.1016/j.jpsychires.2012.01.022. Epub 2012 Feb 18. PMID: 22342346.
[4]. Seo T, Sumiyoshi T, et,al. T-817MA, a novel neurotrophic compound, ameliorates phencyclidine-induced disruption of sensorimotor gating. Psychopharmacology (Berl). 2008 Apr;197(3):457-64. doi: 10.1007/s00213-007-1057-8. Epub 2008 Feb 5. PMID: 18251012.
[5]. Fukushima T, Koide M, et,al.T-817MA, a novel neurotrophic agent, improves sodium nitroprusside-induced mitochondrial dysfunction in cortical neurons. Neurochem Int. 2006 Jan;48(2):124-30. doi: 10.1016/j.neuint.2005.08.012. Epub 2005 Oct 10. PMID: 16219389.
[6]. Fukushima T, Nakamura A, et,al.T-817MA, a neuroprotective agent, attenuates the motor and cognitive impairments associated with neuronal degeneration in P301L tau transgenic mice. Biochem Biophys Res Commun. 2011 Apr 22;407(4):730-4. doi: 10.1016/j.bbrc.2011.03.091. Epub 2011 Mar 31. PMID: 21439944.
[7]. Maekawa H, Matsunobu T, et,al.Protective effect of neurotrophic agent T-817MA against inner ear barotrauma in the guinea pig. J Pharmacol Sci. 2011;117(1):67-70. doi: 10.1254/jphs.11033sc. Epub 2011 Aug 25. PMID: 21869565.
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