标签归档：hemisulfate

Isoprenaline hemisulfate

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Isoprenaline hemisulfate 

Isoprenaline hemisulfate 是一种非选择性的 β-肾上腺素受体激动剂，具有口服活性。Isoprenaline 具有强效的外周血管扩张、支气管扩张和心脏刺激活性。Isoprenaline 可用于心动过缓和支气管哮喘的研究。

Isoprenaline hemisulfate

Isoprenaline hemisulfate Chemical Structure

CAS No. : 299-95-6

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Isoprenaline hemisulfate 的其他形式现货产品:

Isoprenaline hydrochloride

Isoprenaline hemisulfate 相关产品

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•同靶点蛋白产品:

生物活性

Isoprenaline hemisulfate is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma[1][2][3][4][5][6].

IC50 & Target

β adrenergic receptor

 

体外研究
(In Vitro)

Isoprenaline hemisulfate (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[1].
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[2].
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)[3].
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[4].
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[5].
Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Isoprenaline hemisulfate 相关抗体:
体内研究
(In Vivo)

Isoprenaline hemisulfate (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Dogs[1]
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.

Clinical Trial

分子量

260.30

Formula

C11H17NO3.1/2H2O4S
CAS 号

299-95-6
结构分类
  • Alkaloids
  • Other Alkaloids
  • Phenols
  • Polyphenols
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (542 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Degerman E, et al. Evidence that insulin and isoprenaline activate the cGMP-inhibited low-Km cAMP phosphodiesterase in rat fat cells by phosphorylation. Proc Natl Acad Sci U S A. 1990 Jan;87(2):533-7.  [Content Brief]

    [2]. Vannucci SJ, et al. Cell surface accessibility of GLUT4 glucose transporters in insulin-stimulated rat adipose cells. Modulation by isoprenaline and adenosine. Biochem J. 1992 Nov 15;288 (Pt 1):325-30.  [Content Brief]

    [3]. Delpy E, et al. Effects of cyclic GMP elevation on isoprenaline-induced increase in cyclic AMP and relaxation in rat aortic smooth muscle: role of phosphodiesterase 3. Br J Pharmacol. 1996 Oct;119(3):471-8.  [Content Brief]

    [4]. Muller FU, et al. Isoprenaline stimulates gene transcription of the inhibitory G protein alpha-subunit Gi alpha-2 in rat heart. Circ Res. 1993 Mar;72(3):696-700.  [Content Brief]

    [5]. Lei M, et al. Modulation of delayed rectifier potassium current, iK, by isoprenaline in rabbit isolated pacemaker cells. Exp Physiol. 2000 Jan;85(1):27-35.  [Content Brief]

    [6]. M E Conolly, et al. Metabolism of isoprenaline in dog and man. Br J Pharmacol  [Content Brief]

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