Alprenolol ((RS)-Alprenolol)
(Synonyms: 阿普洛尔; (RS)-Alprenolol; dl-Alprenolol) 目录号 : GC32905
A non-selective β-AR and 5-HT receptor antagonist
Cas No.:13655-52-2
Sample solution is provided at 25 µL, 10mM.
Alprenolol is a non-selective β-adrenergic receptor (β-AR) antagonist that is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT1B.1,2 It binds to β1-, β2-, and β3-ARs expressed in CHO cells (Kds = 15, 0.91, and 117 nM, respectively, for the human receptors) and to 5-HT1A and 5-HT1B receptors in rat hippocampal and striatal membranes (Kis = 34 and 134 nM, respectively).1,2 In vivo, alprenolol (40 mg/kg, i.v.) completely blocks the hyperactivity response of rats to 2-PCPA and L-tryptophan.3 Alprenolol (10 μg, i.v.) inhibits decreases in heart rate and left ventricular systolic pressure induced by the β2-AR antagonist ICI 118551 in transgenic mice overexpressing the β2-AR.4 It also reduces the level of abnormal prion fibrils (PrPSc) in the brain of mice intracerebrally infected with prion disease to less than 20% of control levels when administered in drinking water at a dose of 50 mg/L.5
1.Baker, J.G.The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptorsBr. J. Pharmacol.144(3)317-322(2005) 2.Langlois, M., Brémont, B., Rousselle, D., et al.Structural analysis by the comparative molecular field analysis method of the affinity of β-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptorsEur. J. Pharmacol.244(1)77-87(1993) 3.Costain, D.W., and Green, A.R.β-Adrenoceptor antagonists inhibit the behavioural responses of rats to increased brain 5-hydroxytryptamineBr. J. Pharmacol.64(2)193-200(1978) 4.Bond, R.A., Leff, P., Johnson, T.D., et al.Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptorNature374(6519)272-276(1995) 5.Miyazaki, Y., Ishikawa, T., Kamatari, Y.O., et al.Identification of alprenolol hydrochloride as an anti-prion compound using surface plasmon resonance imagingMol. Neurobiol.(2018)
Cas No. | 13655-52-2 | SDF | |
别名 | 阿普洛尔; (RS)-Alprenolol; dl-Alprenolol | ||
Canonical SMILES | OC(COC1=CC=CC=C1CC=C)CNC(C)C | ||
分子式 | C15H23NO2 | 分子量 | 249.35 |
溶解度 | DMSO : ≥ 100 mg/mL (401.04 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 4.0104 mL | 20.0521 mL | 40.1043 mL |
5 mM | 0.8021 mL | 4.0104 mL | 8.0209 mL |
10 mM | 0.401 mL | 2.0052 mL | 4.0104 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet