| Name | Xanomeline |
| Description | Xanomeline (LY-246708) is a functionally selective M1/M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites. |
| In vitro | In binding studies pre-incubating cells for one hour with 1 μM xanomeline, but not carbachol, reduced N-[3H]methylscopolamine saturation binding affinity but not maximal receptor density in cells
[1]. |
| In vivo | Animal studies have shown the role of M4 and M1 receptors in modulating psychotic and behavioral disturbances and correction of negative and/or cognitive symptoms, respectively. The time to reach maximum plasma concentration (Tmax) for xanomeline is 2.5 hours, and maximum plasma concentration following xanomeline 150mg is 13.8ng/mL. Xanomeline is widely distributed, including to the CNS in animal studies, and the majority of the drug is excreted via the kidneys within 24 hours of administration[2]. |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (3.55 mM), Sonication is recommended.
DMSO : 4.5 mg/mL (15.99 mM), Sonication is recommended.
|
| Keywords | Xanomeline | mAChR M4 | mAChR M1 | LY246708 | LY 246708 |
| Inhibitors Related | Adiphenine hydrochloride | Levamisole hydrochloride | Ethyl (triphenylphosphoranylidene) acetate | Urethane | Hexamethonium Bromide | Ribavirin | Adenine | Mitotane | Choline chloride | Propoxur | N,N-Dicyclohexylcarbodiimide | Arecoline |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Anti-Alzheimer's Disease Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | FDA-Approved Drug Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library |
United States
