General
Preferred name
XANOMELINE
Synonyms
Xanomeline oxalate ()
LY246708 ()
LY246708 oxalate ()
LY-246708 ()
LY246708 tartrate ()
LY-246708 tartrate ()
LY 246708 tartrate ()
Xanomeline tartrate ()
[11C]xanomeline ()
Xanomeline (tartrate) ()
Xanomeline (oxalate) ()
LY 246708 (tartrate) ()
LY246708 (oxalate) ()
5-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1-methyl-1,2,3,6-tetrahydropyridine ()
Xanomelina ()
LY-246708 FREE BASE ()
[11C]xanomeline ()
LY-246708 TARTRATE ()
Xanomeline (+)-l-hydrogen tartrate ()
LY246708 TARTRATE ()
Xanomeline Tartaric Acid ()
Xanomeline tartrate component of cobenfy ()
P&D ID
PD047532
CAS
141064-23-5
131986-45-3
1018845-70-9
152854-19-8
Tags
available
drug candidate
drug
Drug indication
Discovery agent
Schizophrenia
Parkinson disease
Drug Status
approved
investigational
Max Phase
4.0
First approval
2024
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer¡¯s disease[1].
PRICE
42
DESCRIPTION
Xanomeline is a muscarinic receptor agonist, with preference for the M1 and M4 receptor subtypes . It also has antagonist activity at 5-HT2 receptors, and agonist activity at 5-HT1 receptors . Xanomeline was investigated for potential to improve cognition in Alzheimer's disease (AD) patients, but activation of muscarinic receptors in the gastrointestinal tract caused severe nausea and diarrhoea, and this adverse effect led to discontinuation of xanomeline's clinical development for AD.
(GtoPdb)
DESCRIPTION
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia[1][2].
PRICE
54
DESCRIPTION
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].
PRICE
59
DESCRIPTION
Selective NOP antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Functionally selective M1 agonist
(Tocriscreen Plus)
DESCRIPTION
Muscarinic receptors are G protein-coupled acetylcholine receptors that play diverse roles. Xanomeline oxalate is a potent agonist of muscarinic acetylcholine receptors (EC50 values are 0.3, 92.5, 5, 52, and 42 nM for M1, M2, M3, M4, and M5, respectively). It has antipsychotic-like activities in rats and Cebus monkeys. M1 selective agonists, like Xanomeline oxalate, enhance memory function and has utility in treating Alzheimer's Disease.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Xanomeline oxalate (LY246708 oxalate), a potent and selective muscarinic receptor agonist (SMRA), effectively stimulates in vivo phosphoinositide hydrolysis. It is a valuable compound for Alzheimer's disease research.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Xanomeline is a Muscarinic M1 and M4 receptor agonist under the development of Eli Lilly, though it is also known to act as a M5 receptor antagonist. Xanomeline has been shown to have reasonable efficacy for the treatment of schizophrenia symptoms although gastrointestinal side effects led to a high drop-out rate in clinical trials. Recent studies showed robust improvements in verbal learning and short-term memory associated with xanomeline treatment. In Dec 1998, Phaes-III clinical trials for Alzheimer's disease in USA was discontinued.
(BOC Sciences Bioactive Compounds)
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.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Xanomeline tartrate (LY 246708 tartrate) is an M1 and M4 mAChR agonist with antipsychotic-like activity that improves cognition and can be used in studies of schizophrenia and Alzheimer's disease.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
1
Compound Sets
25
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
JUMP-Target 1 Compound Set
Ki Database
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
65
Molecular Weight
281.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
1
cLogP
3.22
TPSA
38.25
Fraction CSP3
0.71
Chiral centers
0.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Target
muscarinic receptor
mAChR M1
mAChR M4
CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR6, HTR7
CHRM2
mAChR
Primary Target
M1 Receptors
MOA
Agonist
Muscarinic M1 receptor agonist
Muscarinic M4 receptor agonist
Muscarinic M5 receptor agonist
Cholinergic Muscarinic 1-4 agonist
acetylcholine receptor agonist
Member status
member
Pathway
Neuroscience
GPCR/G protein
Neuronal Signaling
Solubility
Soluble in DMSO
Source data
