152854-19-8

152854-19-8 structure

Name: Xanomeline tartrate
Chemical Name: (2R,3R)-2,3-dihydroxybutanedioic acid,3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole
CAS Number: 152854-19-8
Molecular Formula: C₁₈H₂₉N₃O₇S
Molecular Weight: 431.50400
Catalog: Signaling Pathways GPCR/G Protein mAChR
Create Date: 2017-12-11 03:36:21
Modify Date: 2024-01-09 16:13:47
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].

Name	(2R,3R)-2,3-dihydroxybutanedioic acid,3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole
Synonyms	Memcor Xanomeline tartrate (USAN) Xanomeline tartrate

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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> mAChR Signaling Pathways >> GPCR/G Protein >> mAChR Research Areas >> Neurological Disease
Target	M1/M4[1]
In Vitro	Xanomeline (LY 246708) (0.1-10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline (LY 246708) shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (LY 246708) (＞1 μM) has a prolonged engagement with the receptor and produces a persistent receptor activation leading to a sustained suppression of the M-current[1].
In Vivo	Xanomeline (LY 246708) (0.5-3 mg/kg; s.c.; 1-3 hours) induces salivation and vomiting in some monkeys[3]. Xanomeline (LY 246708) shows functional dopamine antagonism and an antipsychotic-like profile[3]. Xanomeline (LY 246708) inhibits D-amphetamine- and (−)-apomorphine-induced behavior and do not cause extrapyramidal side effects[3]. Animal Model: Male Cebus apella monkeys[3] Dosage: 0.5-3 mg/kg Administration: s.c.; 1-3 hours Result: Induced salivation and vomiting in some monkeys.
References	[1]. Kreir M, et al. Role of Kv7.2/Kv7.3 and M1 muscarinic receptors in the regulation of neuronal excitability in hiPSC-derived neurons. Eur J Pharmacol. 2019;858:172474. [2]. Shekhar A, et al. Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry. 2008;165(8):1033-1039. [3]. Andersen MB, et al. The muscarinic M1/M4 receptor agonist xanomeline exhibits antipsychotic-like activity in Cebus apella monkeys. Neuropsychopharmacology. 2003;28(6):1168-1175.

Boiling Point	397ºC at 760 mmHg
Molecular Formula	C₁₈H₂₉N₃O₇S
Molecular Weight	431.50400
Flash Point	193.9ºC
Exact Mass	431.17300
PSA	181.55000
LogP	1.03140
Vapour Pressure	1.64E-06mmHg at 25°C

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