| Identification | Back Directory | [Name]
LY 246708 tartrate | [CAS]
152854-19-8 | [Synonyms]
Sarnomil tartrate
LY 246708 tartrate
xanomeline tartrat
Xanomeline tartrate
(+)-L-Hydrogen tartrate
Zhan Nuo Meilin Tartrate
3-(Hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole (2R,3R)-2,3-dihydroxysuccinate | [Molecular Formula]
C18H29N3O7S | [MOL File]
152854-19-8.mol | [Molecular Weight]
431.504 |
| Chemical Properties | Back Directory | [Melting point ]
95.5° | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (45 mg/ml) or Water (70 mg/ml) | [form ]
solid | [color ]
Off-white | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 2 months. | [InChIKey]
SJSVWTMVMBGIHQ-LREBCSMRSA-N |
| Hazard Information | Back Directory | [Description]
Xanomeline tartrate (152854-19-8) functionally-selective M1 muscarinic receptor agonist, EC50=0.3, 92.5, 5, 52 and 42 nM for M1, M2, M3, M4 and M5 respectively.1,2 Displays positive cognitive and behavioral effects in schizophrenia and Alzheimer’s disease.3 Suppresses proinflammatory cytokine responses and improves survival in sepsis.4 Displays potent analgesic activity in rodent models of chronic inflammatory and neuropathic pain.5 | [Uses]
Alzheimer’s disease treatment (cholinergic agonist). | [in vivo]
Xanomeline (LY 246708) (0.5-3 mg/kg; s.c.; 1-3 hours) induces salivation and vomiting in some monkeys[3].
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Xanomeline (LY 246708) shows functional dopamine antagonism and an antipsychotic-like profile[3].
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Xanomeline (LY 246708) inhibits D-amphetamine- and (?)-apomorphine-induced behavior and do not cause extrapyramidal side effects[3]. | Animal Model: | Male Cebus apella monkeys[3] | | Dosage: | 0.5-3 mg/kg | | Administration: | s.c.; 1-3 hours | | Result: | Induced salivation and vomiting in some monkeys. |
| [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] J JAKUBÍK. Importance and prospects for design of selective muscarinic agonists.[J]. Physiological research, 2008, 57 Suppl 3: S39-S47. DOI:10.33549/physiolres.931449
[3] AARON M. BENDER Craig W L Carrie K Jones. Classics in Chemical Neuroscience: Xanomeline[J]. ACS Chemical Neuroscience, 2017, 8 3: 435-443. DOI:10.1021/acschemneuro.7b00001
[4] MAURICIO ROSAS-BALLINA . Xanomeline suppresses excessive pro-inflammatory cytokine responses through neural signal-mediated pathways and improves survival in lethal inflammation[J]. Brain, Behavior, and Immunity, 2015, 44: Pages 19-27. DOI:10.1016/j.bbi.2014.07.010
[5] GIOVANNI MARTINO . The M1/M4 preferring agonist xanomeline is analgesic in rodent models of chronic inflammatory and neuropathic pain via central site of action[J]. PAIN®, 2011, 152 12: Pages 2852-2860. DOI:10.1016/j.pain.2011.09.017 |
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