Azumolene

Names

[ Name ]:
Azumolene

[Synonym ]:
Azumolenum
Azumolenum [Latin]
1-[5-(4-bromo-phenyl)-oxazol-2-ylmethyleneamino]-imidazolidine-2,4-dione
Azumolene
Azumoleno
Azumolene [INN]
1-(((5-(4-bromophenyl)-2-oxazolyl)methylene)amino)-2,4-imidazolidinedione
UNII-5U7IO9CV80
Azumoleno [Spanish]

Biological Activity

[Description]:

Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Metabolic Disease

[In Vitro]

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[2].

[In Vivo]

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[1].

[References]

[1]. G C Leslie, et al. The effect of EU4093 (azumolene sodium) on the contraction of intrafusal muscle in the soleus muscle of the anaesthetized rat. Br J Pharmacol. 1989 Aug;97(4):1151-6.

[2]. Viktor Yarotskyy, et al. Accelerated activation of SOCE current in myotubes from two mouse models of anesthetic- and heat-induced sudden death. PLoS One. 2013 Oct 15;8(10):e77633.

Chemical & Physical Properties

[ Density]:
1.79g/cm3

[ Molecular Formula ]:
C₁₃H₉BrN₄O₃

[ Molecular Weight ]:
349.14000

[ Exact Mass ]:
347.98600

[ PSA ]:
87.80000

[ LogP ]:
2.25650

[ Index of Refraction ]:
1.739

Safety Information

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

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