Diphemanil Methylsulfate

製品コードS4034 バッチS403401

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

C20H24N.CH3O4S
分子量 389.51 CAS No. 62-97-5
Solubility (25°C)* 体外 DMSO 25 mg/mL (64.18 mM)
Water 18 mg/mL (46.21 mM)
Ethanol Insoluble
* <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 Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
in vitro Diphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. In addition to its well known antimuscarinic effects, Diphemanil Methylsulfate also possesses direct smooth muscle spasmolytic activity.
in vivo The pharmacokinetic experiments show that absorption of diphemanil methylsulphate is slow (tmax = 2 to 4 h), the mean half-life is 8.35 h, and the amount of the drug recovered in urine within 48 h ranges from 0.6 to 7.4% of the administered dose[1]. Poorly absorbed from the gastrointestinal tract with an absolute bioavailability of 15 to 25%.

プロトコル(参考用のみ)

キナーゼアッセイ Measurements of tension changes in isolated guinea-pig trachealis muscle strips
Female Hartley strain guinea pigs weighing 300 to 600 g are sacrificed by an i.p. injection of urethan, 5 g/kg. The trachea is removed, trimmed free of excess tissue and cut in a spiral fashion, each turn separated by 3 to 4 cartilage segments. Each strip is approximately halved and each half mounted in a waterjacketed (37-39°C) 10 mL tissue bath containing a modified Krebs-Henseleit solution of the following composition (grams per liter): NaCl,6.92; KC1, 0.35; CaCl2•2H2O, 0.28; KH2PO4, 0.16; MgSO4•7H2O, 0.29; NaHCO3, 2.1; and dextrose, 2.1 in distilled, deionized water. The tissue bath and stock salt solutions are aerated with a mixture of 95% O2 and 5% CO2. Strips are allowed to equilibrate for 90 to 120 mm before addition of drugs and washings are made at 15-mm intervals during this period. Resting tension is adjusted to 1 g. Contractions are recorded isometrically using Grass FTO3 force-displacement transducers in conjunction with a Hewlett-Packard 7404A oscillographic recorder. Drugs are evaluated for its ability to reverse agonist-induced contractures. Methacholine bromide and ionic potassium are used as the agonists and are added to the bathing fluid in concentrations which produced approximately 85% of the maximum response which the tissue is capable of generating. These concentraions ( ca. 5 μM for methacholine and 35 mM for potassium) are determined for each individual trachealis muscle strip. After the contraction induced by the agonist has stabilized, cumulative doses of the antagonist are delivered to the bath and the maximal decrease in tension is recorded at each concentration. The percentage of relaxation of the agonist-induced contraction is plotted vs. concentration of antagonist. An estimate of the median effective concentration (EC50) of each antagonist is determined from a regression line calculated for the concentration-response data.

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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