A β1-adrenergic receptor partial agonist (EC50 = 80 nM for the generation of cAMP in neonatal rat cardiomyocyte cultures); increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM); increases heart rate in beagle dogs (ED50 = 3.2 µg/kg) and a rat model of spontaneous heart failure (ED50 = 6 µg/kg)

Xamoterol (hemifumarate) – 25 mg

Brand:
Cayman
CAS:
73210-73-8
Storage:
-20
UN-No:
Non-Hazardous - /

Xamoterol is a partial agonist of β1-adrenergic receptors (β1-ARs) with an EC50 value of 80 nM for the generation of cyclic AMP (cAMP) in neonatal rat cardiomyocyte cultures.{41648} It increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM).{41649} In vivo, xamoterol increases heart rate in beagle dogs (ED50 = 3.2 µg/kg) and in a rat model of spontaneous heart failure (ED50 = 6 µg/kg), an effect that is reversed by the selective β1-AR antagonist betaxolol (Item No. 18625) but not the selective β2-AR antagonist ICI 118551 (Item No. 15591).{41648,41647} Formulations containing xamoterol have been used in the treatment of heart failure.  

 

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Description

A β1-adrenergic receptor partial agonist (EC50 = 80 nM for the generation of cAMP in neonatal rat cardiomyocyte cultures); increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM); increases heart rate in beagle dogs (ED50 = 3.2 µg/kg) and a rat model of spontaneous heart failure (ED50 = 6 µg/kg)

Formal name: N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-4-morpholinecarboxamide, (E)-2-butenedioate (2:1)

Synonyms:  ICI 118587

Molecular weight: 397.4

CAS: 73210-73-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Heart|Arrhythmia

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