| Identification | Back Directory | [Name]
3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridineoxalate | [CAS]
141064-23-5 | [Synonyms]
Lumeron
LY246708 oxalate
Xanomeline oxalate
Xanomeline oxalate salt
LY246708;MEMCOR;LUMERON
3-(3-Hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine oxalate
3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridineoxalate
3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine ethanedioate (1:1) | [Molecular Formula]
C14H23N3OS.C2H2O4 | [MDL Number]
MFCD12828778 | [MOL File]
141064-23-5.mol | [Molecular Weight]
371 |
| Chemical Properties | Back Directory | [Melting point ]
148-150℃ | [storage temp. ]
Desiccate at +4°C | [solubility ]
DMF: 1.6 mg/ml; DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. | [Uses]
Xanomeline oxalate is a functionally selective mAChR M1 agonist. | [in vivo]
Xanomeline robustly stimulates in vivo PI hydrolysis and the effect is blocked by muscarinic antagonists, demonstrating mediation by muscarinic receptors. In mice the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 54 μmole/kg in hippocampus. And in rats the ED100 for Xanomeline-induced stimulation of [3H]-IP accumulation is 8.1 μmole/kg in hippocampus[1]. | Animal Model: | Male CF1 mice weighing 18-20 g are injected [3H]-myoinositol[1] | | Dosage: | 8.1-81 μmole/kg | | Administration: | S.c. injections; 1 h prior to killing and 1 h after the administration | | Result: | Increased accumulation in a dose-related manner up to 130%, 75%, 60% above lithium levels in hippocampus, cortex and neostriatum, respectively. And did not increase accumulation of [3H]-IP in the brain stem.
Induced salivation, tremor and hypothermia in mice with the ED50 of 13.7±0.8 μmole/kg.
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| Animal Model: | Rats are injected [3H]-myoinositol[1] | | Dosage: | 2.7-81 μmole/kg | | Administration: | S.c. injections; 1 h prior to killing and 1 h after the administration | | Result: | Increased [3H]-IP formation dose dependently in hippocampus up to 221% above lithium control. |
| [storage]
Store at -20°C | [References]
[1] JULIA N. HEINRICH . Pharmacological comparison of muscarinic ligands: Historical versus more recent muscarinic M1-preferring receptor agonists[J]. European journal of pharmacology, 2009, 605 1: Pages 53-56. DOI: 10.1016/j.ejphar.2008.12.044
[2] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[3] MAIBRITT B ANDERSEN. The Muscarinic M1/M4 Receptor Agonist Xanomeline Exhibits Antipsychotic-Like Activity in Cebus apella Monkeys[J]. Neuropsychopharmacology, 2003, 28 6: 1168-1175. DOI: 10.1038/sj.npp.1300151
[4] MESSER W S. The utility of muscarinic agonists in the treatment of alzheimer’s disease[J]. Journal of Molecular Neuroscience, 2002, 19 1-2: 187-193. DOI: 10.1007/s12031-002-0031-5 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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