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).
Heinrich et al. (2009), Pharmacological Comparison of Muscarininc Ligands: Historical Versus more Recent Muscarinic M1-preferring Receptor Agonists; Eur. J. Pharmacol., 605 53
Jakubik et al. (2008), Importance and prospects for design of selective muscarinic agonists; Physiol. Res., 57 Suppl. 3 S39
Bender et al. (2017), Classics in Chemical Neuroscience: Xanomeline; ACS Chem. Neurosci, 8 435
Rosas-Ballina et al. (2015), Xanomeline Suppresses Excessive Pro-Inflammatory Cytokine Responses Through Neural Signal-Mediated Pathways and Improves Survival in Lethal Inflammation; Brain Behav. Immun., 44 19
Martino et al. (2011), The M1/M4 Preferring Agonist Xanomeline Is Analgesic in Rodent Models of Chronic Inflammatory and Neuropathic Pain via Central Site of Action; Pain, 152 2852
