トラザミド 化学特性,用途語,生産方法
外観
白色～わずかにうすい黄色, 結晶性粉末～粉末
溶解性
本品0.1g＋アセトン10mlでほとんど澄明アセトンにやや溶けやすく、エタノール(95)に溶けにくく、水にほとんど溶けない。
用途
糖尿病の基礎研究。
効能
糖尿病治療薬, 血糖降下薬, スルホニル尿素受容体作動薬
説明
Tolazamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (K
IR6.2; IC
50 = 4.2 μM in HEK293 cells transfected with the human receptor). It has no effect on glucose uptake in L6 rat skeletal muscle cells when used at a concentration of 0.6 mg/mL but enhances glucose uptake two-fold when used in combination with insulin.
In vivo, tolazamide (128 mg/kg) reduces glomerulosclerosis and albumin excretion in a rat model of insulin-dependent diabetes induced by streptozotocin . Formulations containing tolazamide have been used in the treatment of type 2 diabetes.
化学的特性
White Solid
使用
Labelled Tolazamide, an antidiabetic.
定義
ChEBI: An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.
一般的な説明
Tolazamide is N-[[(hexahydro-1H-azepin-1-yl)amino]carbonyl]-4-methylbenzenesulfonamide; or 1-(hexahydro-1H-azepin-1-yl)-3-(p-tolylsulfonyl)urea; or 1-(4-methylphenylsulfonyl)-3-(hexahydro-1H-azepin-1-yl)urea (generic).Tolazamide incorporates a fully saturated azepine moietythat is but weakly basic, with a pKa of～3.
32 The pKa of thesulfonylurea group lies within the typical range; thus, inareas of the duodenum wherein the pH falls within the rangeof 4 to 5, the uncharged form of the drug is the predominantspecies, and its lipophilicity lends to rapid absorption bypassive diffusion.
空気と水の反応
TOLAZAMIDE may be sensitive to prolonged exposure to air. Insoluble in water.
反応プロフィール
TOLAZAMIDE is an amide. Amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as P2O5 or SOCl2 generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx). TOLAZAMIDE is incompatible with acids. .
火災危険
Flash point data for TOLAZAMIDE are not available; however, TOLAZAMIDE is probably combustible.
トラザミド 上流と下流の製品情報
原材料
準備製品