ChemicalBook Product Catalog API Nervous system drugs Drug Metabolism in Human Brain AVex-73

AVex-73

Product NameAVex-73
CAS195615-83-9
MFC19H23NO
MW281.39
EINECS
MOL File195615-83-9.mol

Chemical Properties

solubility	DMF: 30 mg/ml DMSO: Slightly soluble Ethanol: 30 mg/ml
form	Solid
color	White to off-white

Usage And Synthesis

Uses

Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome[1].

in vivo

Blarcamesine (10 mg/kg, 30 mg/kg; p.o.; daily; for 6.5 weeks) ameliorates motor deficits in Mecp2 HET mice with chronic administration^[1].
Blarcamesine ameliorates acoustic startle deficit in Mecp2 HET mice^[1].
Blarcamesine reverses deficits in visual acuity in older Mecp2 HET mice using the optokinetic response^[1].
Blarcamesine produces minimal effects on body weight gain in Mecp2 HET mice^[1].

Animal Model:	Female Mecp2^tm1.1Bird/J HET (C57 background) mice^[1]
Dosage:	10 mg/kg, 30 mg/kg
Administration:	Oral administration, daily, for 6.5 weeks
Result:	Reverse the deficits observed in the HET animals.

IC 50

Sigma 1 Receptor

References

[1] Walter E Kaufmann, et al. ANAVEX2-73 (Blarcamesine), a Sigma-1 Receptor Agonist, Ameliorates Neurologic Impairments in a Mouse Model of Rett Syndrome. Pharmacol Biochem Behav . 2019 Dec;187:172796. DOI:10.1016/j.pbb.2019.172796
[2] VALENTINE LAHMY. Mitochondrial protection by the mixed muscarinic/σ1 ligand ANAVEX2-73, a tetrahydrofuran derivative, in Aβ25-35 peptide-injected mice, a nontransgenic Alzheimer’s disease model.[J]. Frontiers in Cellular Neuroscience, 2015: 463. DOI: 10.3389/fncel.2014.00463
[3] VALENTINE LAHMY. Blockade of Tau Hyperphosphorylation and Aβ1–42 Generation by the Aminotetrahydrofuran Derivative ANAVEX2-73, a Mixed Muscarinic and σ1 Receptor Agonist, in a Nontransgenic Mouse Model of Alzheimer’s Disease[J]. Neuropsychopharmacology, 2013, 38 9: 1706-1723. DOI: 10.1038/npp.2013.70

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