Xamoterol hemifumarate Struktur

Bis[N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]morpholin-4-carboxamid]fumarat

Bezeichnung:Bis[N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]morpholin-4-carboxamid]fumarat

Englisch Name:Xamoterol hemifumarate

CBNumberCB0249700

SummenformelC36H54N6O14

Molgewicht794.85

Synonyma

Bis[N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]morpholin-4-carboxamid]fumarat

Bis[N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]morpholin-4-carboxamid]fumarat physikalisch-chemischer Eigenschaften

Sicherheit

S-Sätze:	22-24/25
WGK Germany	3

Gefahreninformationscode (GHS)

S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
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.
Beschreibung
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)
Verwenden
Xamoterol Hemifumarate, is a β1-adrenoceptor-selective partial agonist.
Verwenden
Stimulant (cardiac).
Trademarks
Corwin
Biologische Aktivität
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).
Lager
Store at RT