Xanomeline oxalate

Research use only, not for human use.

Xanomeline oxalate (LY246708, NNC 110232) is a potent, specific M1 muscarinic agonist with functional selectivity for M1 receptor.

Xanomeline oxalate (LY246708, NNC 110232) is a potent, specific M1 muscarinic agonist with functional selectivity for M1 receptor (binding IC50 of 6 pM in the rabbit vas deferens); displays low affinity for M2 receptors in guinea pig atria (EC50=3 uM); xanomeline increases striatal levels of dopamine metabolites, presumably by acting at M1 heteroreceptors on dopamine neurons to increase dopamine release in vivo; inhibits ex vivo binding of muscarinic radioligands to homogenates of brain and the inhibition of ex vivo binding occurred in the same dose range as increases in DOPAC levels; xanomeline is selective agonist for M1 over M2 and M3 receptors in vivo in rats.Alzheimer Disease Phase 3 Discontinued.

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Animal Model:Male CF1 mice weighing 18-20 g are injected [3H]-myoinositol Dosage:8.1-81 μmole/kg Administration:S.c. injections; 1 h prior to killing and 1 h after the administration Result:Increased accumulation in a dose-related manner up to 130%, 75%, 60% above lithium levels in hippocampus, cortex and neostriatum, respectively. And did not increase accumulation of [3H]-IP in the brain stem.Induced salivation, tremor and hypothermia in mice with the ED50 of 13.7±0.8 μmole/kg.Animal Model:Rats are injected [3H]-myoinositol Dosage:2.7-81 μmole/kg Administration:S.c. injections; 1 h prior to killing and 1 h after the administration Result:Increased [3H]-IP formation dose dependently in hippocampus up to 221% above lithium control.

LY246708 | LY-246708 | NNC 110232

GPCR/G Protein

mAChR

mAChR

Neurological Disease

Alzheimer Disease

141064-23-5

371.5

C16H25N3O5S

>98% (HPLC)

10 mM in DMSO

CCCCCCOC1=NSN=C1C2=CCCN(C2)C.C(=O)(C(=O)O)O

Pyridine, 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl-, ethanedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years