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Doxapram hydrochloride hydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Doxapram hydrochloride hydrate图片
CAS NO:7081-53-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Doxapram hydrochloride hydrate 抑制 TASK-1、TASK-3、TASK-1/TASK-3 异二聚体通道功能,EC50 分别为 410 nM、37 μM、9 μM。
Cas No.7081-53-0
别名多沙普仑盐酸一水合物
化学名1-ethyl-4-(2-morpholin-4-ylethyl)-3,3-diphenylpyrrolidin-2-one;hydrate;hydrochloride
Canonical SMILESCCN1CC(C(C1=O)(C2=CC=CC=C2)C3=CC=CC=C3)CCN4CCOCC4.O.C
分子式C24H30N2O2.HCl.H2O
分子量432.98
溶解度≥ 20.05mg/mL in DMSO with gentle warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.Target: Potassium ChannelDoxapram is a respiratory stimulant. Doxapram (15-150 microM) also evoked 3H overflow in a concentration dependent manner, and doxapram-evoked release was inhibited by the Ca2+ channel blocker nifedipine (5 microM). Analysis of released tritiated compounds suggested that doxapram preferentially stimulated the release of dopamine. Our results indicate that the mechanism of action of doxapram shares similarities with that of hypoxia in the carotid body [1]. Doxapram (1-100 microM) caused rapid, reversible and dose-dependent inhibitions of K+ currents recorded in type I cells (IC50 approximately 13 microM). doxapram was also seen to directly inhibit Ca(2+)-independent K+ currents. Doxapram was a more potent inhibitor of the Ca(2+)-activated K+ currents recorded under control conditions. Doxapram (10 microM) was without effect on L-type Ca2+ channel currents recorded under conditions where K+ channel activity was minimized and was also without significant effect on K+ currents recorded in the neuronal cell line NG-108 15, suggesting a selective effect on carotid body type I cells. The effects of doxapram on type I cells show similarities to those of the physiological stimuli of the carotid body, suggesting that doxapram may share a similar mechanism of action in stimulating the intact organ [2].

References:
[1]. Cotten JF, et al. The ventilatory stimulant doxapram inhibits TASK tandem pore (K2P) potassium channel function but does not affect minimum alveolar anesthetic concentration. Anesth Analg, 2006, 102(3), 779-785.
[2]. Anderson-Beck, R., et al., Doxapram stimulates dopamine release from the intact rat carotid body in vitro. Neurosci Lett, 1995. 187(1): p. 25-8.
[3]. Peers, C., Effects of doxapram on ionic currents recorded in isolated type I cells of the neonatal rat carotid body. Brain Res, 1991. 568(1-2): p. 116-22.