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Isoprenaline hemisulfate
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Isoprenaline hemisulfate
CAS No. : 299-95-6
MCE 站:Isoprenaline hemisulfate
产品活性:Isoprenaline hemisulfate 是一种非选择性的 β-肾上腺素能受体(β-adrenergic receptor)激动剂,具有有效的外周血管扩张剂,支气管扩张剂和心脏刺激活性。
研究领域:GPCR/G Protein | Neuronal Signaling | Metabolic Enzyme/Protease
作用靶点:Adrenergic Receptor | Endogenous Metabolite
In Vitro: 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 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.
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