Isoprenaline (Synonyms:异丙肾上腺素;Novodrin;Norisodrine)
目录号 : KM32610 CAS No. : 7683-59-2 纯度 : 99%

Isoprenaline 是一种具有口服活性的非选择性 β-肾上腺素受体激动剂。该化合物作为有效的外周血管扩张剂和支气管扩张剂,可用于心动过缓和支气管哮喘的研究,并用于治疗心脏传导阻滞和心动过缓。

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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性

Isoprenaline(Norisodrine) is a non-selective and orally active β-adrenoceptor agonist.Isoproterenol is a potent peripheral vasodilator and bronchodilator.Isoproterenol can be used in the study of bradycardia and bronchial asthma for the treatment of heart block, bradycardia.

体外研究

Isoprenaline (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase (cAMP-PDE) activity by about 100% in intact rat fat cells.

Isoprenaline inhibits insulin-stimulated glucose transport activity in rat adipocytes. Isoprenaline, in the absence of adenosine, promotes a time-dependent (t1/2 approximately 2 min) decrease in the accessibility of insulin-stimulated cell surface GLUT4 of > 50%, which directly correlated with the observed inhibition of transport activity.

Isoprenaline (5 nM and 10 μM) increases cyclic AMP levels and this effect is potentiated by cilostamide (10 mM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO).

Isoprenaline increases the transcriptional activity of Gi alpha-2 gene to 140% of the control value, whereas gene specific hybridization for Gs alpha remains unchanged.

Isoprenaline (20 nM) increases the amplitude of total iK and causes a negative shift of approximately 10 mV in the activation curve for iK, both in the absence and in the presence of 300 nM nisoldipine to block the L-type Ca2+ current.

Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells.

体内研究

Isoprenaline (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs.

 

Animal Model: Dogs
Dosage: 0.27-0. 64 μg/kg
Administration: oral
Result: Excreted largely unchanged in urine, only one-third of the radioactivity in urine was in the form of the O-methyl metabolite.
Showed plasma radioactivity was almost entirely as conjugated isoprenaline and this metabolite accounted for more than 80% of radioactivity in urine.
. Showed heart rate returned to base-line values when high plasma concentrations.
 
分子式
C11H17NO3
分子量
211.26
CAS号
7683-59-2
中文名称
异丙肾上腺素
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO: 10 mg/mL (47.34 mM; Need ultrasonic)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 4.7335 mL 23.6675 mL 47.3350 mL
5 mM 0.9467 mL 4.7335 mL 9.4670 mL
10 mM 0.4734 mL 2.3668 mL 4.7335 mL
*

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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-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。

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