Xamoterol hemifumarate Property

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

Safety Statements 

22-24/25

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

Xamoterol hemifumarate Chemical Properties,Usage,Production

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