FSL0350

Structure

• InChI=1S/C25H29I2NO3.ClH/c1-4-7-11-22-23(18-10-8-9-12-21(18)31-22)24(29)17-15-19(26)25(20(27)16-17)30-14-13-28(5-2)6-3;/h8-10,12,15-16H,4-7,11,13-14H2,1-3H3;1H
• InChIKey=ITPDYQOUSLNIHG-UHFFFAOYSA-N

Synonyms

• 1951-25-3
• Amiodarone hydrochloride

Origin

Chemically synthesized

Biological activities

The class III antiarrhythmic action partly through blockade of multi channels

Therapeutic

Antiarrhythmic (class III)
Vasodilator

Target

Multi channels (K⁺, Na⁺, Ca²⁺)
PTX-sensitive G protein

Assay information

Blockage of multi channels (IC₅₀ [μM]): ICaL (0.4-5.8), ICaT (2.4), INa (0.1-7.3), IK (6.3), IKNa (1.0), Ito (4.9), IKAch (2.0), IKATP (2.3), INa/Ca (3.3)
Activation of GTPase of reconstituted Gi/Go and Gi2 with EC50 values of 20 μM and 50 μM
Cytotoxicity against PANC1, H9C2, BRL-3A (GI50: 10-50 μM)
Antifungal activity against Heterobasidiomycetes, Ascomycetes, and Hyphomycetes (MIC₅₀: 1-10 μM)

References

• Prog. Med., 31: 761-764 (2011)
• Varbiro G, Toth A, Tapodi A, Veres B, Sumegi B, Gallyas F Jr
  Concentration dependent mitochondrial effect of amiodarone.
  Biochem Pharmacol, 65(7): 1115-1128 (2003)  12663047
• Courchesne WE
  Characterization of a novel, broad-based fungicidal activity for the antiarrhythmic drug amiodarone.
  J Pharmacol Exp Ther, 300(1): 195-199 (2002)  11752116
• Hagelüken A, Nürnberg B, Harhammer R, Grünbaum L, Schunack W, Seifert R
  The class III antiarrhythmic drug amiodarone directly activates pertussis toxin-sensitive G proteins.
  Mol Pharmacol, 47(2): 234-240 (1995)  7870030
• DELTOUR G, BINON F, TONDEUR R, GOLDENBERG C, HENAUX F, SION R, DERAY E, CHARLIER R
  [Studies in the benzofuran series. VI. Coronary-dilating activity of alkylated and aminoalkylated derivatives of 3-benzoylbenzofuran].
  Arch Int Pharmacodyn Ther, 139: 247-254 (1962)  14026835