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抑制剂描述:

产品名称:Isoproterenol Hydrochloride

产品别名:见爱必信官网

英文别名:Isoproterenol Hydrochloride

靶点:Adrenergic Receptor

CAS:51-30-9

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Isoproterenol hydrochloride is a phenethylamine derivative and selective β-AR adrenergic agonist shown to increase cytosolic cAMP. Isoproterenol hydrochloride exhibits promotion of glycogen breakdown and causes bronchodilation and vasorelaxant effects. Also potentially stimulates relaxation in nitric oxide mediated endothelium-dependent smooth muscle. Isoproterenol Hydrochloride is an activator of β2-AR and ERK.

溶解性:Soluble in water (50 mg/ml at 25° C), ethanol (20 mg/ml), methanol, DMSO (50 mg/ml at 25° C), and phosphate buffered saline (50 mM).

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 mM) 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:

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