An internal standard for the quantification of esmolol
Esmolol-d7 is intended for use as an internal standard for the quantification of esmolol by GC- or LC-MS. Esmolol is a β1-adrenergic receptor (β1-AR) antagonist.1 It binds to β1-ARs (Kd = 100 nM in isolated cardiac myocytes) and is 34-fold selective for β1- over β2-ARs.1,2 Esmolol also inhibits L-type Ca2+ currents (ICa.L) and the fast Na+ current (INa) in rat cardiac myocytes (IC50s = 50 and 169 μM, respectively), which results in complete ventricular arrest at concentrations greater than or equal to 1 mM.1 Formulations containing esmolol have been used in the treatment of cardiac arrhythmias, postoperative hypertension, and acute ischemic heart disease, as well as to minimize myocardial contraction during cardiac surgery and attenuate the adrenergic response associated with tracheal intubation.
1.Fallouh, H.B., Bardswell, S.C., McLatchie, L.M., et al.Esmolol cardioplegia: The cellular mechanism of diastolic arrestCardiovasc. Res.87(3)552-560(2010) 2.Jahn, P., Eckrich, B., Schneidrowski, B., et al.β1-adrenoceptor subtype selective antagonism of esmolol and its major metabolite in vitro and in man. Investigations using tricresylphosphate as red blood cell carboxylesterase inhibitorArznei.-Forschung45(5)536-541(1995)
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