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inamrinone
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inamrinone

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Also known as WIN-40680, Inocor, Amcoral, Amrinona, Amrinonum, Amrinone

Amrinone, also known as inamrinone, and sold as Inocor, is a pyridine phosphodiesterase 3 inhibitor. It is a drug that may improve the prognosis in patients with congestive heart failure. Amrinone has been shown to increase the contractions initiated in the heart by high-gain calcium induced calcium release (CICR). The positive inotropic effect of amrinone is mediated by the selective enhancement of high-gain CICR, which contributes to the contraction of myocytes by phosphorylation through cAMP dependent protein kinase A (PKA) and Ca2+ calmodulin kinase pathways.

Research

2,468 papers

via PubMed

Wikidata facts

Mass
187.074562
Show 4 more facts
chemical formula
C₁₀H₉N₃O
defined daily dose
0.5
canonical SMILES
C1=CN=CC=C1C2=CNC(=O)C(=C2)N
Commons category
Amrinone
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~6 min read

Article

11 sections
Contents
  • Actions
  • PDE-III inhibition and cardiac function
  • Indications
  • Effects in congestive heart failure
  • Contraindications
  • Precautions
  • Side effects
  • Amrinone discovery and progression
  • Naming
  • Synthesis
  • References

Amrinone, also known as inamrinone, and sold as Inocor, is a pyridine phosphodiesterase 3 inhibitor. It is a drug that may improve the prognosis in patients with congestive heart failure. Amrinone has been shown to increase the contractions initiated in the heart by high-gain calcium induced calcium release (CICR). The positive inotropic effect of amrinone is mediated by the selective enhancement of high-gain CICR, which contributes to the contraction of myocytes by phosphorylation through cAMP dependent protein kinase A (PKA) and Ca2+ calmodulin kinase pathways.

==Actions== Increases cardiac contractility, vasodilator. Acts by inhibiting the breakdown of both cAMP and cGMP by the phosphodiesterase (PDE3) enzyme. There is a long-standing controversy regarding whether the drug actually increases cardiac contractility in diseased myocardium (and therefore whether it is of any clinical use). The issue has been reviewed extensively by Dr Peter Wilmshurst, one of the first cardiologists and researchers to question the drug's efficacy.

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