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Isoprenaline hemisulfate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Isoprenaline hemisulfate图片
CAS NO:299-95-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

Isoprenaline hemisulfate is a non-selective, orally activeβ-adrenergic receptoragonist. 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-KmcAMP 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].

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].

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

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.