Isoprenaline hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

盐酸异丙肾上腺素是一种非选择性 β-肾上腺素激动剂，结构与肾上腺素相似。

Isoprenaline Hydrochloride is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.(In Vitro):Isoprenaline (Isoproterenol) hydrochloride (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.(In Vivo):Isoprenaline (Isoproterenol) hydrochloride (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs.

Isoprenaline (Isoproterenol) hydrochloride (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.

Isoprenaline (Isoproterenol) hydrochloride (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.

Isoprenaline | NSC 37745 | NSC 89747

Endocrinology/Hormones

Adrenergic Receptor

Adrenergic Receptor| CAMP PDE| PI3K

Cardiovascular Disease

——

51-30-9

247.72

C11H18ClNO3

>98% (HPLC)

Water: 50 mg/mL (201.84 mM); DMSO: 50 mg/mL (201.84 mM)

OC(CNC(C)C)C1=CC=C(O)C(O)=C1.[H]Cl

Benzenemethanol, 3,4-dihydroxy-alpha-(((1-methylethyl)amino)methyl)-, hydrochloride, (+/-)-

(-20℃)

With Ice Pack

≥ 2 years