For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I038384 |
| CAS Number | 152854-19-8 |
| Synonyms | (2S,3S)-2,3-dihydroxybutanedioic acid;3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole |
| Molecular Formula | C18H29N3O7S |
| Purity | ≥95% |
| InChI | InChI=1S/C14H23N3OS.C4H6O6/c1-3-4-5-6-10-18-14-13(15-19-16-14)12-8-7-9-17(2)11-12;5-1(3(7)8)2(6)4(9)10/h8H,3-7,9-11H2,1-2H3;1-2,5-6H,(H,7,8)(H,9,10)/t;1-,2-/m.0/s1 |
| InChIKey | SJSVWTMVMBGIHQ-WUUYCOTASA-N |
| SMILES | CCCCCCOC1=NSN=C1C2=CCCN(C2)C.C(C(C(=O)O)O)(C(=O)O)O |
| 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. |
