ベナゼプリル塩酸塩

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ベナゼプリル塩酸塩 価格

ベナゼプリル塩酸塩 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色, 結晶性粉末～粉末

• 溶解性

  エタノールに溶け、水にやや溶けにくい。

• 用途

  高血圧の研究。

• 用途

  アンジオテンシン変換酵素 （ACE）阻害剤です。アンジオテンシン変換 酵素を阻害し、アンジオテンシンⅡ生成抑制 作用を示します。

• 用途

  アンジオテンシン変換酵素 （ACE-1）阻害剤です。アンジオテンシン変 換酵素を阻害し、アンジオ

• 効能

  血圧降下薬, アンジオテンシン変換酵素(ACE)阻害薬

• 商品名

  チバセン (サンファーマ)

• 説明

  Benazepril hydrochloride is a long-acting and effective angiotensin-converting enzyme (ACE) inhibitor used to treat essential hypertension. It is the hydrochloride salt form of benazepril, which is a prodrug of benazeprilat. After hepatic cleavage of the ester group, benazepril is converted to benazeprilat. In healthy humans, it was well tolerated and showed no phmacokinetic interactions with furosemide, hydrochlorothiazide, chlorthalidone, digoxin, cimetidine, atenolol, or naproxen.

• 化学的特性

  This substance is a white to off-white crystalline powder. It is highly soluble in water, ethanol, and methanol with a solubility of over 100 mg/mL.

• 使用

  Benazepril HCl is an angiotensin-converting enzyme (ACE) inhibitors that is commonly used as a sedative, hypnotic, and antihypertensive medication. Benazepril is used alone or together with other medicines to treat high blood pressure (hypertension). It works by reducing the levels of certain chemicals that cause blood vessels to constrict, allowing for smoother blood flow.

• 定義

  ChEBI: Benazepril hydrochloride is a hydrochloride salt resulting from the reaction of benazepril with 1 mol eq. of hydrogen chloride. It is used as a prodrug for angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure. It has a role as an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor. It contains a benazepril(1+).

• 一般的な説明

  Benazepril is a prodrug of the angiotensin converting enzyme (ACE) inhibitor benazeprilat . It is metabolized to benazeprilat by hepatic esterases. Benazepril inhibits the in vitro enzymatic activity of partially purified ACE isolated from rabbit lung (IC50 = 2 nM). It decreases the triglyceride and total cholesterol levels in normotensive rats when administered at a dose of 30 mg/kg and decreases aortic atherosclerosis in cholesterol-fed rabbits when administered at a dose of 3 mg/kg per day. Benazepril (0.1-10 mg/kg per day) reduces blood pressure in spontaneously hypertensive rats. It also decreases proteinuria in cats with chronic kidney disease when administered at doses ranging from 0.5 to 1 mg/kg per day. Formulations containing benazepril have been used to treat hypertension, congestive heart failure, and chronic kidney disease in both human and veterinary medicine.

• 生物活性

  Non-peptide angiotensin-converting enzyme (ACE) inhibitor. Reduces blood pressure and myocardial hypertrophy in spontaneous hypertensive rats.

• 合成

  Benazepril hydrochloride is prepared through the following steps:
  Step 1: Preparation of (R)-ethyl 2-hydroxy-4-phenylbutyrate using ethyl 2-oxo-4-phenylbutyrate as a raw material and cinchonidine as a chiral ligand through asymmetric catalytic hydrogenation under high pressure.
  Step 2: The intermediate obtained from step 1 reacts with p-nitrobenzenesulfonyl chloride or trifluoromethanesulfonic anhydride to obtain the corresponding sulfonate.
  Step 3: The sulfonate obtained from step 2 undergoes nucleophilic substitution and salt hydrolysis with (3S)-3-amino-2,3,4,5-tetrahydro-2-oxo-1H-benzazepine-1-tert-butyl acetate to obtain benazepril hydrochloride.
  This procedure has been described in detail in documents such as CN110835319A, US4785089, WO02076375, EP206993, and CN105061312.

• Mode of action

  The mechanism of action of benazepril is to inhibit the activity of the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II Label, thereby alleviating a series of symptoms caused by angiotensin (elevated blood pressure, increased excitatory heart rate caused by vasodilation, insufficient cardiac output, etc.).

• 参考文献

  https://www.novartis.com/us-en/sites/novartis_us/files/lotrel.pdf
  https://dailymed.nlm.nih.gov/dailymed/lookup.cfmsetid=a216253b-27cb-42ef-b5a8-67fb05aafb88
  Extrapyramidal side effect of donepezil hydrochloride in an elderly patient DOI: 10.1097/MD.0000000000019443
  Use of convertible isocyanides for the synthesis of benazepril hydrochloride DOI: 10.1007/s12039-021-01892-8

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