Xamoterol hemifumarate Chemical Properties

Melting point:

168-169° (dec)

storage temp. 

Store at RT

solubility 

H₂O: 10 mg/mL at 60 °C, soluble

form 

solid

color 

white

CAS DataBase Reference

73210-73-8

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

Xamoterol hemifumarate Usage And Synthesis

Description

Xamoterol fumarate is a cardioselective partial beta-agonist, the first of its class to be developed for use in heart failure. The main advantage of xamoterol fumarate as a cardiotonic lies in the fact that its beta-blocking effect exerted during high sympathetic drive will protect the heart from overstimulation. It is claimed to be a viable but safer alternative to digoxin.

Description

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. It increases spontaneous contraction of isolated rat right atria (EC₅₀ = 4.67 nM). 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 but not the selective β₂-AR antagonist ICI 118551 . Formulations containing xamoterol have been used in the treatment of heart failure.

Originator

ICI (United Kingdom)

Uses

Xamoterol Hemifumarate, is a β1-adrenoceptor-selective partial agonist.

Uses

Stimulant (cardiac).

brand name

Corwin

Biological Activity

β 1 -adrenoceptor-selective partial agonist (pA 2 values are 7.4-7.8 and 5.2-6.2 at β 1 - and β 2 -adrenoceptors respectively).

storage

Store at RT

Xamoterol hemifumarate(73210-73-8)Related Product Information

• Fumaric acid
• XAMOTEROL HEMIFUMARATE
• Xamoterol hemifumarate