Doxapram HCl

製品コードS4037 バッチS403702

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H30N2O2.HCl.H2O
分子量 432.98 CAS No. 7081-53-0
Solubility (25°C)* 体外 DMSO 86 mg/mL (198.62 mM)
Water 86 mg/mL (198.62 mM)
Ethanol 86 mg/mL (198.62 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.
in vitro 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. [1]
in vivo 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%.[2]

プロトコル(参考用のみ)

キナーゼアッセイ Two-electrode voltage clamp technique
All experiments are performed using frog Ringer’s solution as perfusate (in mM): NaCl 115, KCl 2.5, CaCl2 1.8, and HEPES 10, with a pH value of 7.4. The high potassium frog Ringer’s substituted 115 mM of KCl for 115 mM of NaCl. Oocytes are impaled with 0.1– 0.3 MΩ glass electrodes and studied in a 25-μL recording chamber under continuous perfusion. Time course data are collected by clamping the transmembrane potential at - 60 mV and averaging the outward current over a 1-s duration square-wave + 60 mV voltage pulse using a 1.5 s interpulse interval. Signals are low-pass filtered (50–100 Hz) and digitized (100–1000 Hz) before analysis
動物実験 動物モデル male Japanese white rabbits
投薬量 0.25 mg/kg/h, 0.50 mg/kg/h
投与方法 Infusion

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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