product name Esmolol HCl
Description: Esmolol (also known as ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms. Esmolol contains one asymmetric centre and exists as an enantiomeric pair, the (-)-enantiomer is active and the (+)-enantiomer is inactive, which is analogous to other P-blockers that have an oxypropranolamine nucleus. Esmolol has a rapid onset and offset of activity, the primary site of activity of Esmolol is on sinus node and atrioventricular (AV) nodal conduction systems.
References: Clin Pharmacokinet. 1995 Mar;28(3):190-202; Crit Care Med. 2005 Oct;33(10):2294-301.
331.83
Formula
C16H25NO4.HCl
CAS No.
81161-17-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (198.9 mM)
Water: 66 mg/mL (198.9 mM)
Ethanol: 66 mg/mL (198.9 mM)
Solubility (In vivo)
Synonyms
ASL8052
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19398903
| In Vitro |
In vitro activity: Esmolol contains one asymmetric centre and exists as an enantiomeric pair, the (-)-enantiomer is active and the (+)-enantiomer is inactive, which is analogous to other P-blockers that have an oxypropranolamine nucleus. Esmolol has a rapid onset and offset of activity, the primary site of activity of Esmolol is on sinus node and atrioventricular (AV) nodal conduction systems. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Esmolol (20 mg/kg) infusion in sepsis improves oxygen utilization of myocardium and preserves myocardial function in septic rats. Esmolol (5 mg/kg, i.v.) produces a dose-dependent decrease in heart rate (HR) in rabbits, with the maximum percent reductions of 13%. Esmolol (5 mg/kg, i.v.) produces a dose-dependent decrease in mean arterial pressure (MAP) in rabbits, with the maximum percent reductions of 38.2%. Esmolol (300 mg/kg) significantly decreases the heart rate, rate-pressure product, left ventricular contraction, cardiac output, and relative refractory period of the right ventricle, suppresses the AV nodal conduction, and increases the effective refractory period of the right ventricle and the preload of the left ventricle in canine. Esmolol (300 mg/kg) significantly reduces the isoproterenol-induced increase in heart rate and ventricular contraction in canine. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Pharmacokinet. 1995 Mar;28(3):190-202; Crit Care Med. 2005 Oct;33(10):2294-301. |
Related Posts
product name Esmolol HCl
Description: Esmolol (also known as ASL8052) is a cardioselective b-blocker, used to control rapid heartbeats or abnormal heart rhythms. Esmolol contains one asymmetric centre and exists as an enantiomeric pair, the (-)-enantiomer is active and the (+)-enantiomer is inactive, which is analogous to other P-blockers that have an oxypropranolamine nucleus. Esmolol has a rapid onset and offset of activity, the primary site of activity of Esmolol is on sinus node and atrioventricular (AV) nodal conduction systems.
References: Clin Pharmacokinet. 1995 Mar;28(3):190-202; Crit Care Med. 2005 Oct;33(10):2294-301.
331.83
Formula
C16H25NO4.HCl
CAS No.
81161-17-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (198.9 mM)
Water: 66 mg/mL (198.9 mM)
Ethanol: 66 mg/mL (198.9 mM)
Solubility (In vivo)
Synonyms
ASL8052
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19398903
| In Vitro |
In vitro activity: Esmolol contains one asymmetric centre and exists as an enantiomeric pair, the (-)-enantiomer is active and the (+)-enantiomer is inactive, which is analogous to other P-blockers that have an oxypropranolamine nucleus. Esmolol has a rapid onset and offset of activity, the primary site of activity of Esmolol is on sinus node and atrioventricular (AV) nodal conduction systems. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Esmolol (20 mg/kg) infusion in sepsis improves oxygen utilization of myocardium and preserves myocardial function in septic rats. Esmolol (5 mg/kg, i.v.) produces a dose-dependent decrease in heart rate (HR) in rabbits, with the maximum percent reductions of 13%. Esmolol (5 mg/kg, i.v.) produces a dose-dependent decrease in mean arterial pressure (MAP) in rabbits, with the maximum percent reductions of 38.2%. Esmolol (300 mg/kg) significantly decreases the heart rate, rate-pressure product, left ventricular contraction, cardiac output, and relative refractory period of the right ventricle, suppresses the AV nodal conduction, and increases the effective refractory period of the right ventricle and the preload of the left ventricle in canine. Esmolol (300 mg/kg) significantly reduces the isoproterenol-induced increase in heart rate and ventricular contraction in canine. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Pharmacokinet. 1995 Mar;28(3):190-202; Crit Care Med. 2005 Oct;33(10):2294-301. |