Xamoterol hemifumarate

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)

The Uses of Xamoterol hemifumarate

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

The Uses of Xamoterol hemifumarate

Stimulant (cardiac).

What are the applications of Application

Xamoterol is an authentic β1-adrenoceptor (β1-AR) agonist that has been shown to mimic the autoantibody effect on rat atria β1-AR apoptosis

What are the applications of Application

Xamoterol hemifumarate is a β1-adrenoceptor-selective partial agonist

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