Isoprenaline 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 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]. |
体外研究
(In Vitro) | Isoprenaline (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].
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体内研究
(In Vivo) | Isoprenaline (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.
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Showed heart rate returned to base-line values when high plasma concentrations. |
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| 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. |
