Doxapram hydrochloride monohydrate,7081-53-0

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产品名称：Doxapram hydrochloride monohydrate

产品别名：多沙普仑盐酸一水合物

英文别名：Doxapram hydrochloride monohydrate

靶点：TASK-1 ，TASK-1/TASK-3 heterodimeric ，TASK-3

CAS：7081-53-0

纯度：>98%

外观：白色结晶性粉末

保存方法：-20°C 冷藏长期储存,常温运输及临时存放

描述：

Doxapram hydrochloride inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

溶解性：Ethanol ：2 mg/mL (4.61 mM)
DMSO ：81 mg/mL (187.1 mM)
Water ：23 mg/mL (53.1 mM)

体外研究：

Doxapram inhibits both TASK-1 and TASK-3 function in a dose dependent manner. Doxapram inhibition at both hyperpolarized and depolarized potentials, as well as effects independent of extracellular potassium concentration. It is said that the carboxy terminal domain of TASK-1 is important to doxapram inhibition. Doxapram also inhibits TRESK, TASK-2, and TREK-1 but at significantly larger concentrations (EC50s of 240 μM, 460 μM, and >1 mM, respectively). Doxapram has no effect on MAC for halothane.

体内研究：Doxapram is an analeptic agent. The respiratory stimulant action is manifested by an increase in tidal volume associated with a slight increase in respiratory rate. A pressor response may result following Doxapram administration.The mean half-life is 3.4 h (range 2.4-4.1h), the mean apparent volume of distribution is 1.5 mg/kg and the whole body clearance is 370 mL/min. Enteric-coated capsules of doxapram base are absorbed rapidly after an initial delay, and the systemic availability is about 60%.

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