PeptideDB

Xanomeline tartrate

CAS: 152854-19-8 F: C18H29N3O7S W: 431.50

Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (
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Bioactivity Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia[1][2][3].
Target M1/M4
Invitro Xanomeline (LY 246708) (0.1-10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline (LY 246708) shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (LY 246708) (>1 μM) has a prolonged engagement with the receptor and produces a persistent receptor activation leading to a sustained suppression of the M-current[1].
In Vivo Xanomeline (LY 246708) (0.5-3 mg/kg; s.c.; 1-3 hours) induces salivation and vomiting in some monkeys[3].Xanomeline (LY 246708) shows functional dopamine antagonism and an antipsychotic-like profile[3].Xanomeline (LY 246708) inhibits D-amphetamine- and (−)-apomorphine-induced behavior and do not cause extrapyramidal side effects[3]. Animal Model:
Name Xanomeline tartrate
CAS 152854-19-8
Formula C18H29N3O7S
Molar Mass 431.50
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [1]. Kreir M, et al. Role of Kv7.2/Kv7.3 and M1 muscarinic receptors in the regulation of neuronal excitability in hiPSC-derived neurons. Eur J Pharmacol. 2019;858:172474. [2]. Shekhar A, et al. Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry. 2008;165(8):1033-1039. [3]. Andersen MB, et al. The muscarinic M1/M4 receptor agonist xanomeline exhibits antipsychotic-like activity in Cebus apella monkeys. Neuropsychopharmacology. 2003;28(6):1168-1175.