Home Neuronal Signaling GABA Receptor activator alpha-Asarone

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alpha-Asarone GABA Receptor activator

Cat.No.S4772

Alpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects.
alpha-Asarone GABA Receptor activator Chemical Structure

Chemical Structure

Molecular Weight: 208.25

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Quality Control

Batch: S477201 DMSO]41 mg/mL]false]]]false]]]false Purity: 99.76%
99.76

Chemical Information, Storage & Stability

Molecular Weight 208.25 Formula

C12H16O3

 Storage (From the date of receipt)
CAS No. 2883-98-9 Download SDF Storage of Stock Solutions

Synonyms trans-Asarone Smiles CC=CC1=CC(=C(C=C1OC)OC)OC

Solubility

In vitro
Batch:

DMSO : 41 mg/mL (196.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

In vitro
α-asarone possesses an endothelium-dependent vasodilation property, and in normal HUVEC-derived EA.hy926 cells, α-asarone has been shown to upregulate the expression of phosphorylated eNOS (Ser1177), causing an increase in the production of NO. It protects against injury to endothelial cells by attenuating Ang II-mediated changes in intracellular ROS/NO.
In vivo
Alpha-Asarone treatment alleviates locomotor hyperactivity in Fmr1 KO mice. It improves m1 mAChR expression and up-regulates the ACh levels in the striatum. Its treatment also attenuates the increased striatal AChE activity in Fmr1 KO mice. Alpha-asarone has been reported to have a beneficial effect in cognitive impairment induced by dysfunction of the cholinergic system in the brain through inhibition of AChE activity. Of all the doses tested (2, 10, 40, 80 and 120 mg/kg) in rats, 10 mg/kg α-Asarone improves the quality of sleep, as indicated by an increased NREM bout duration, reduced arousal index, and decreased bout frequencies of NREM sleep and wakefulness. A marginal decrease in the hypothalamic and body temperatures is also observed. Higher doses, on the other hand, not only reduce the quantity and quality of sleep, but also produce hypothermia.
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