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131986-45-3

131986-45-3 structure
131986-45-3 structure
  • Name: Xanomeline
  • Chemical Name: xanomeline
  • CAS Number: 131986-45-3
  • Molecular Formula: C14H23N3OS
  • Molecular Weight: 281.41700
  • Catalog: API Respiratory medication Asthma
  • Create Date: 2018-09-23 06:22:00
  • Modify Date: 2024-01-02 07:51:51
  • 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].

Name xanomeline
Synonyms 3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole
3-(Hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole
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].
Related Catalog
Target

M1/M4[1][2]

In Vitro Xanomeline (0.1~10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (>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 (0.5~3 mg/kg; s.c.; 1~3 hours) induces salivation and vomiting in some monkeys[3]. Xanomeline shows functional dopamine antagonism and an antipsychotic-like profile.Xanomeline inhibits D-amphetamine- and (−)-apomorphine-induced behavior and do not cause extrapyramidal side effects[3]. Animal Model: Male Cebus apella monkeys 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.

Density 1.101 g/cm3
Boiling Point 397ºC at 760 mmHg
Molecular Formula C14H23N3OS
Molecular Weight 281.41700
Flash Point 193.9ºC
Exact Mass 281.15600
PSA 66.49000
LogP 3.15400
Appearance off-white
Vapour Pressure 1.64E-06mmHg at 25°C
Index of Refraction 1.537
Storage condition 2-8°C
Water Solubility H2O: soluble10mg/mL, clear (warmed)
HS Code 2934999090
Precursor  2

DownStream  0

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%