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外観
白色〜ほとんど白色, 結晶〜粉末
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溶解性
アセトン, クロロホルムに易溶。エタノールに可溶。水に不溶。エーテルに難溶。
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用途
薬理研究用。
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用途
スルホニル尿素剤（SU剤）です。 膵β細胞膜のSU受容体と結合してカリウム チャンネルを閉じることによりインスリン分 泌を促進します。
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用途
スルホニル尿素剤（SU 剤）です。
膵β 細胞膜のSU 受容体と結合してカリウム
チャネルを閉じることによりインスリン分泌
を促進します。
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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
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化学的特性
White or almost white, crystalline powder.
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使用
Tolbutamide, have been used in a cDNA microarray assay to probe changes in gene expression in HepG2 cells upon their administration. It has been utilized to counteract insulin activity in a patch-clamp investigation of ATP sensitive K+ channels in mouse pancreatic β-cells. The activity of various biotransformation enzymes in cultured primary rat proximal tubular cells in the presence of tolbutamide and other compounds has been studied.
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定義
ChEBI: An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.
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一般的な説明
Tolbutamide is N-[(butylamino)carbonyl]-4-methylbenzenesulfonamide;or 1-butyl-3-(p-tolylsulfonyl)urea (Orinase,generic). Orinase Diagnostic was the sodium salt, which isfreely soluble in water for injection, but this product was discontinuedc. 2000.
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空気と水の反応
Insoluble in water.
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反応プロフィール
TOLBUTAMIDE 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). TOLBUTAMIDE is incompatible with acids. .
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火災危険
Flash point data for TOLBUTAMIDE are not available. TOLBUTAMIDE is probably combustible.
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作用機序
Tolbutamide is one of the most widely used antidiabetic agents. Its action is preferably
connected with stimulatory action of β-cells in the pancreas, which results in intensive
insulin secretion.
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臨床応用
Tolbutamide should be used only when the diabetic patientis an adult or shows adult-onset diabetes, and the patientshould adhere to dietary restrictions.
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安全性プロファイル
Moderately toxic by
ingestion and several other routes. A human
teratogen. Human reproductive effects by
ingestion and possibly other routes:
stillbirth, developmental abnormalities of
the cardlovascular (circulatory) system and
urogenital system, and unspecified neonatal
effects. Human systemic effects by
ingestion: nausea or vomiting, hypoglycemia.
Other experimental teratogenic and
reproductive effects. Mutation data
reported. Implicated in aplastic anemia.
When heated to decomposition it emits very
toxic fumes of NO, and SOx.
