An active metabolite of esmolol
货号:ajcx28258
CAS:83356-60-9
分子式:C15H23NO4 • HCl
分子量：317.8
溶解度:DMF: insol,DMSO: insol,Ethanol: insol,PBS (pH 7.2): 5 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Esmolol acid is an active metabolite of the β₁-adrenergic receptor (β₁-AR) antagonist esmolol .¹It is formed from esmololviahydrolysis by a red blood cell esterase. Esmolol acid inhibits isoproterenol-induced increases in the beating rate of isolated guinea pig right atria (pA₂= 3.73) and prevents tachycardia and hypotension induced by isoproterenol in anesthetized dogs in a dose-dependent manner.²It is also a potential impurity in commercial preparations of esmolol.³

1.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 inhibitorArzneimittelforschung45(5)536-541(1995) 2.Shaffer, J.E., Quon, C.Y., and Gorczynski, R.J.β-adrenoreceptor antagonist potency and pharmacodynamics of ASL-8123, the primary acid metabolite of esmololJ. Cardiovasc. Pharmacol.11(2)187-192(1988) 3.Sahadev Reddy, M., Reddy, M.S.N., Rajan, S.T., et al.Structural identification and characterization of impurities in esmolol hydrochlorideDer Pharma Chem.8(4)296-300(2016)