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Isoprenaline hydrochloride

CAS No. : 51-30-9

MCE 国际站：Isoprenaline hydrochloride

产品活性：Isoprenaline (Isoproterenol) hydrochloride 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。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Metabolic Enzyme/Protease

作用靶点：Adrenergic Receptor  |  Endogenous Metabolite

In Vitro: Isoprenaline (Isoproterenol) hydrochloride (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-K_m 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.

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