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My CartCAS：81161-17-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 81161-17-3 |
| Name | Esmolol Hydrochloride |
| Molecular Formula | C16H26ClNO4 |
| Molecular Weight | 331.83 |
| Solubility | Soluble in Water/DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00941432 |
| SMILES | CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O.Cl |
| InChIKey | GEKNCWBANDDJJL-UHFFFAOYSA-N |
| InChI | InChI=1S/C16H25NO4.ClH/c1-12(2)17-10-14(18)11-21-15-7-4-13(5-8-15)6-9-16(19)20-3;/h4-5，7-8，12，14，17-18H，6，9-11H2，1-3H3;1H |
| PubChem CID | 104769 |
| Target Point | Adrenergic Receptor |
| Passage | Endocrinology & Hormones;GPCR & G Protein；Neuronal Signaling |
| Background | It is a beta adrenergic receptor inhibitor. |
| Biological Activity | Esmolol Hydrochloride 是一种肾上腺素受体阻滞剂，用于控制心跳急或异常心率节律。[1] |
| In Vitro | 艾司洛尔含有一个不对称中心且以一对对映体的形式存在，(-)- 对映体是有活性的，(+)- 对映异构体是无活性的，这与其他具有一个oxypropranolamine细胞核的P-抑制剂类似。Esmolol具有迅速起效和失活的功能，Esmolol的主要活性部位是窦房结和房室结传导系统。[1] |
| In Vivo | 脓毒症患者输注艾司洛尔可提高心肌的氧利用率并保护心肌功能。与对照组相比，输注艾司洛尔不会导致动脉乳酸水平升高，但会降低肿瘤坏死因子-α的浓度(p < .05)。 与对照组相比，经艾司洛尔治疗的大鼠在整个研究期间的心输出量和心脏效率均显著提高(p < .05)。[2] 艾司洛尔均产生剂量依赖性HR降低，艾司洛尔5 mg*kg(-1)对HR的最大降低百分比为-14.0 +/- 0.9%和-13.9 +/- 1.4%)。艾司洛尔产生了剂量依赖性的MAP下降，MAP的最大降幅为-38.2 +/- 3.2%。[3] 艾司洛尔(300 mg/kg)作用于犬类，可以显著降低心脏速率，心率收缩压乘积，左室收缩，心输出量，右心室相对不应期，抑制房室结传导，并提高右心室不应期的效率和左心室的前负荷。此外，Esmolol(300 mg/kg)作用于犬类，还可显著降低异丙基肾上腺素诱导的心率增加和心室收缩。[4] |
| Animal Experiment | 盲肠结扎穿孔后，将大鼠随机分为对照组(生理盐水2 mL/hr，n = 11)、低剂量艾司洛尔组(10 mg/kg/hr，n = 10)、高剂量艾司洛尔组(20 mg/kg/hr，n = 10)。[2] 采用静脉滴注不同剂量艾司洛尔(0.5、1.5、5.0 mg*kg(-1))，比较其对大鼠心率(HR)、平均动脉压(MAP)和肾交感神经活动(RSNA)的影响。[3] |
| Data Literature Source | [1]. Wiest D. Esmolol. A review of its therapeutic efficacy and pharmacokinetic characteristics. Clin Pharmacokinet. 1995 Mar;28(3):190-202. [2]. Suzuki T，et al. Infusion of the beta-adrenergic blocker esmolol attenuates myocardial dysfunction in septic rats. Crit Care Med. 2005 Oct;33(10):2294-301. [3]. Sasao J，et al. In rabbits，landiolol，a new ultra-short-acting beta-blocker，exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol. Can J Anaesth. 2001 Nov;48(10):985-9. [4]. Sugiyama A，et al. Electrophysiologic，cardiohemodynamic and beta-blocking actions of a new ultra-short-acting beta-blocker，ONO-1101，assessed by the in vivo canine model in comparison with esmolol. J Cardiovasc Pharmacol. 1999 Jul;34(1):70-7. |
| Unit | Bottle |
| Specification | 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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