Azumolene

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Azumolene是一种直接作用的骨骼肌松弛剂，其结构与丹曲林钠相似，即丹曲林钠的对硝基苯基被对溴苯基取代。

Azumolene1.EU4093 (azumolene sodium) is a direct acting, skeletal muscle relaxant with structural similarities to dantrolene sodium in that the para-nitro phenyl group of dantrolene sodium is replaced by a para-bromo phenyl group.?2.?The effect of EU4093 on the twitch of the intact rat soleus preparation is nearly maximal at a dose of 20 mg kg-1.?This dose of EU4093 reduces the amplitude of the twitch to 31.9% of the control value.?By comparison, dantrolene sodium reduced the twitch amplitude to 31.3% of the control value at a dose of 5 mg kg-1.?3.?The contraction of intrafusal muscle as measured by the response of spindle afferent discharge was also reduced by EU4093.?4.?The most significant difference between the effect of EU4093 and dantrolene sodium on the contraction of intrafusal muscle was that EU4093 had an appreciable depressant action at high stimulation frequencies at which dantrolene sodium had only a minimal relaxant effect on the intrafusal muscle contraction.

Pretreatment with 20 μM Azumolene for 1-2 min inhibits SOCE activated by subsequent addition of caffeine and ryanodine to promote RyR-dependent sarcoplasmic reticulum Ca2+ store depletion in mouse myotubes and adult muscle fibers.

The effect of Azumolene (EU4093) on the twitch of the intact rat soleus preparation is nearly maximal at a dose of 20 mg/kg. This dose of Azumolene reduces the amplitude of the twitch to 31.9% of the control value. The contraction of intrafusal muscle as measured by the response of spindle afferent discharge is also reduced by Azumolene.

EU4093 free base

GPCR/G Protein

Calcium Channel

Calcium Channel

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64748-79-4

349.14

C13H9BrN4O3

>98% (HPLC)

DMSO:13.89 mg/mL (39.78 mM; Need ultrasonic)

O=C1NC(CN1/N=C/C2=NC=C(C3=CC=C(Br)C=C3)O2)=O

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(-20℃)

With Ice Pack

≥ 2 years