Xanomeline oxalate - CAS 141064-23-5
Catalog number: 141064-23-5
Category: Inhibitor
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Molecular Formula:
C16H25N3O5S
Molecular Weight:
371.45
COA:
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Targets:
mAChR
Description:
Muscarinic receptors are G protein-coupled acetylcholine receptors that play diverse roles. Xanomeline oxalate is a potent agonist of muscarinic acetylcholine receptors (EC50 values are 0.3, 92.5, 5, 52, and 42 nM for M1, M2, M3, M4, and M5, respectively). It has antipsychotic-like activities in rats and Cebus monkeys. M1 selective agonists, like Xanomeline oxalate, enhance memory function and has utility in treating Alzheimer’s Disease.
Purity:
>98%
Synonyms:
LY246708; LY 246708; LY-246708; Memcor; Lumeron
MSDS:
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InChIKey:
ZJOUESNWCLASJP-UHFFFAOYSA-N
InChI:
InChI=1S/C14H23N3OS.C2H2O4/c1-3-4-5-6-10-18-14-13(15-19-16-14)12-8-7-9-17(2)11-12;3-1(4)2(5)6/h8H,3-7,9-11H2,1-2H3;(H,3,4)(H,5,6)
Canonical SMILES:
CCCCCCOC1=NSN=C1C2=CCCN(C2)C.C(=O)(C(=O)O)O
1.Attenuation of neurodegenerative phenotypes in Alzheimer-like presenilin 1/presenilin 2 conditional double knockout mice by EUK1001, a promising derivative of xanomeline.
Wang D1, Yang L, Su J, Niu Y, Lei X, Xiong J, Cao X, Hu Y, Mei B, Hu JF. Biochem Biophys Res Commun. 2011 Jul 1;410(2):229-34. doi: 10.1016/j.bbrc.2011.05.120. Epub 2011 May 27.
The M1/M4-preferring muscarinic agonist xanomeline was found to have some benefit in the treatment of the memory impairment of Alzheimer's disease (AD), but side effects precluded further development. EUK1001, a fluorinated derivative of xanomeline, because of greater affinity for M1 muscarinic receptors, is likely to have a significantly better side effect profile than xanomeline. We have now studied the effects of 3-month chronic administration of EUK1001 and xanomeline (0.5mg/kg/day) in AD-like presenilin 1/presenilin 2 conditional double knockout (PS cDKO) mice. Only EUK1001 was found to significantly ameliorate the deficit in recognition memory. Histological analysis demonstrated partial attenuation of the brain atrophy in EUK1001-treated PS cDKO mice and minimal effect in the xanomeline-treated mice. Both compounds effectively suppressed the elevation of brain tau phosphorylation in the PS cDKO mice, but neither inhibited the increased inflammatory responses.
2.A novel derivative of xanomeline improved memory function in aged mice.
Cui YH1, Si W, Yin L, An SM, Jin J, Deng SN, Cao XH. Neurosci Bull. 2008 Aug;24(4):251-7. doi: 10.1007/s12264-008-0204-5.
OBJECTIVE: To characterize the function of a new xanomeline-derived M1 agonist, 3-[3-(3-florophenyl-2-propyn-1-ylthio)-1,2,5-thiadiazol-4-yl]-1,2,5,6- tetrahydro-1-methylpyridine Oxalate (EUK1001), the acute toxicity and the effects on synaptic plasticity and cognition of EUK1001 were evaluated.
3.3-[3-(3-florophenyl-2-propyn-1-ylthio)-1, 2, 5-thiadiazol-4-yl]-1, 2, 5, 6-tetrahydro-1- methylpyridine oxalate, a novel xanomeline derivative, improves neural cells proliferation and survival in adult mice.
Zhang X1, Gong Q2, Zhang S2, Wang L2, Hu Y3, Shen H4, Dong S3. Neural Regen Res. 2012 Jan 5;7(1):24-30. doi: 10.3969/j.issn.1673-5374.2012.01.004.
The present study analyzed the influence of 3-[3-(3-florophenyl-2-propyn-1-ylthio)-1, 2, 5-thiadiazol-4-yl]-1, 2, 5, 6-tetrahydro-1-methylpyridine oxalate (EUK1001), a novel xanomeline derivative of the M1/M4 receptor agonist, on hippocampal neurogenesis in adult C57BL6 mice. Results showed that 15-day EUK1001 treatment via intraperitoneal injection promoted neural cell proliferation in the dentate gyrus, although cell differentiation did not change. The majority of bromodeoxyuridine-positive cells co-expressed the immature neuronal marker doublecortin. In addition, the level of neurogenesis in the subventricular zone was not altered. Brain-derived neurotrophic factor mRNA expression was up-regulated following EUK1001 treatment, but no change was observed in expression of camp-responsive element binding protein 1, paired box gene 6, vascular endothelial growth factor alpha, neurogenic differentiation factor 1, and wingless-related mouse mammary tumor virus integration site 3A mRNA.
4.A novel derivative of xanomeline improves fear cognition in aged mice.
Si W1, Zhang X, Niu Y, Yu H, Lei X, Chen H, Cao X. Neurosci Lett. 2010 Apr 5;473(2):115-9. doi: 10.1016/j.neulet.2010.02.031. Epub 2010 Feb 21.
The M1/M4 muscarinic acetylcholine receptor agonist xanomeline can significantly improve the cognitive function, but the intolerable side effects limit its clinical usefulness. Our recent study has reported a novel derivative of xanomeline, 3-[3-(3-(3-florophenyl)-2-propyn-1-ylthio)-1,2,5-thiadiazol-4-yl]-1,2,5,6-tetrahydro-1-methylpyridine oxalate (EUK1001), exhibited higher affinity of mAChRs and less side effects relative to xanomeline. In the present study, we further utilized behavioral and electrophysiological techniques to investigate the effects of EUK1001 on fear cognition and hippocampal long-term potentiation (LTP) in aged mice. Behavioral testing showed that 0.1, 0.5 or 1.0mg/kg EUK1001 group, like 1.0mg/kg xanomeline group, exhibited better performance in contextual fear conditioning and passive avoidance test than vehicle-controls. In the cued fear conditioning test, just 0.5 or 1.0, but not 0.1mg/kg EUK1001, significantly enhanced the levels of freezing response.
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CAS 141064-23-5 Xanomeline oxalate

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