152854-19-8

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

Alzheimer’s disease treatment (cholinergic agonist).

[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