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ジアゾキシド

ジアゾキシド 化学構造式
364-98-7
CAS番号.
364-98-7
化学名:
ジアゾキシド
别名:
ヒペルトナルム;プログリセム;7-クロロ-3-メチル-2H-1,2,4-ベンゾチアジアジン1,1-ジオキシド;オイデミン;ジゾキシド;ジアゾキシド;ヒペルスタット;ムタベース;アログリセム;ジアゾキサイド;ジアゾキシド (JAN)
英語化学名:
DIAZOXIDE
英語别名:
Eudemine;Sch-6783;mutabase;srg95213;dizoxide;hyperstat;NSC-64198;proglicem;DIAZOXIDE;Diazoxided
CBNumber:
CB8426893
化学式:
C8H7ClN2O2S
分子量:
230.67
MOL File:
364-98-7.mol

ジアゾキシド 物理性質

融点 :
>310°C
比重(密度) :
1.3767 (rough estimate)
屈折率 :
1.6300 (estimate)
貯蔵温度 :
Store at RT
溶解性:
0.1 M NaOH: soluble
酸解離定数(Pka):
pKa 8.5 (Uncertain)
外見 :
neat
水溶解度 :
Soluble in 0.1M NaOH. Insoluble in water or in methanol.
極大吸収波長 (λmax):
268nm(MeOH)(lit.)
Merck :
14,3004
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  Xn
Rフレーズ  22-36/37/38
Sフレーズ  22-26-36
WGK Germany  3
RTECS 番号 DK8185000
HSコード  2934990002
絵表示(GHS)
注意喚起語 Warning
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 P264, P270, P301+P312, P330, P501
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 P264, P280, P302+P352, P321,P332+P313, P362
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 P264, P280, P305+P351+P338,P337+P313P
H335 呼吸器への刺激のおそれ 特定標的臓器毒性、単回暴露; 気道刺激性 3 警告
注意書き
P261 粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。
P304+P340 吸入した場合:空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。
P405 施錠して保管すること。

ジアゾキシド 価格 もっと(18)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01FLC047209 ジアゾキシド
Diazoxide
364-98-7 500mg ¥38900 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01FLC047209 ジアゾキシド
Diazoxide
364-98-7 1g ¥58700 2018-12-26 購入
東京化成工業 D5402 ジアゾキシド >98.0%(HPLC)(T)
Diazoxide >98.0%(HPLC)(T)
364-98-7 250mg ¥5400 2018-12-04 購入
東京化成工業 D5402 ジアゾキシド >98.0%(HPLC)(T)
Diazoxide >98.0%(HPLC)(T)
364-98-7 1g ¥16000 2018-12-04 購入
Sigma-Aldrich Japan 1186000 ジアゾキシド United States Pharmacopeia (USP) Reference Standard
Diazoxide United States Pharmacopeia (USP) Reference Standard
364-98-7 200mg ¥70900 2018-12-25 購入

ジアゾキシド 化学特性,用途語,生産方法

外観

白色~うすい褐色, 結晶~粉末

溶解性

メタノールに溶ける。

用途

薬理研究用。

効能

低血糖治療薬, 血圧降下薬, ATP感受性カリウムチャネル開口薬

商品名

ジアゾキシド (MSD)

化学的特性

White Solid

使用

wound healing agent

使用

Diazoxide reduces status epilepticus neuron damage in diabetes.

定義

ChEBI: A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the oncentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.

brand name

Hyperstat (Schering); Proglycem (Baker Norton).

生物学の機能

Diazoxide (Hyperstat) is chemically similar to the thiazide diuretics. It is devoid of diuretic activity and causes Na+ and water retention. Diazoxide is a very potent vasodilator and is available only for intravenous use in the treatment of hypertensive emergencies. The mechanism by which diazoxide relaxes vascular smooth muscle is related to its ability to activate potassium channels and produce a hyperpolarization of the cell membrane.

一般的な説明

Diazoxide is 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine-1,1-dioxide , and is currentlyavailable in the United States only as a 50-mg/mLoral suspension (Proglycem); discontinued formulations includedcapsules for oral administration, and injectable formsthat typically found use for indications other than hypoglycemicconditions. Diazoxide is a cyclic benzenesulfonamide,although the free acid in solution can exist in threetautomeric forms, and the 4H tautomer most likely predominatesto a very high proportion. Partly because of theadditional nitrogen in the quinazoline ring structure, themolecule is somewhat more acidic (pKa~8.4, 8.6)than benzenesulfonamide (pKa~10).

一般的な説明

Diazoxide is used as the sodium salt of7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide(Hyperstat IV). Diazoxide lowers peripheral vascular resistance,increases cardiac output, and does not compromiserenal blood flow.
This is a des-sulfamoyl analog of the benzothiazine diureticsand has a close structural similarity to chlorothiazide. Itwas developed intentionally to increase the antihypertensiveaction of the thiazides and to minimize the diuretic effect.

生物活性

Antihypertensive, activates ATP-dependent K + channels. Induces activation of PKC ε , an intermediate in the opening of mitoK ATP channels, results in cardioprotection against hypoxia-induced death. Blocks desensitization of AMPA receptors.

薬理学

The hemodynamic effects of diazoxide are similar to those of hydralazine and minoxidil. It produces direct relaxation of arteriolar smooth muscle with little effect on capacitance beds. Since it does not impair cardiovascular reflexes, orthostasis is not a problem. Its administration is, however, associated with a reflex increase in cardiac output that partially counters its antihypertensive effects. Propranolol and other -blockers potentiate the vasodilating properties of the drug. Diazoxide has no direct action on the heart. Although renal blood flow and glomerular filtration may fall transiently, they generally return to predrug levels within an hour.

臨床応用

Diazoxide is used by intravenous injection as a rapidly acting antihypertensiveagent for emergency reduction of blood pressurein hospitalized patients with accelerated or malignanthypertension. More than 90% is bound to serum protein, andcaution is needed when it is used in conjunction with otherprotein-bound drugs that may be displaced by diazoxide.The injection is given rapidly by the intravenous route toensure maximal effect. The initial dose is usually 1 mg/kg ofbody weight, with a second dose given if the first injectiondoes not lower blood pressure satisfactorily within 30 minutes.Further doses may be given at 4- to 24-hour intervalsif needed. Oral antihypertensive therapy is begun as soon aspossible.

臨床応用

In contrast to the acute clinical uses of glucagon, diazoxidefinds use in chronic hypoglycemic conditions: inoperableislet cell adenoma or carcinomas, extrapancreatic malignanciesof insulin-secreting cells, or islet cell hyperplasias. Inchildren, additional indications include congenital hyperinsulinemia124and leucine sensitivity. Experimentally, diazoxideis among an array of ATP-sensitive potassium channel openersbeing studied for intermittently bringing aboutβ-cell rest.

副作用

Since diazoxide is not often used for long-term treatment, toxicities associated with chronic use are rare.The chief concern is the side effects associated with the increased workload on the heart, which may precipitate myocardial ischemia and Na+ and water retention. These undesirable effects can be controlled by concurrent therapy with a β-blocker and a diuretic.
Diazoxide may cause hyperglycemia, especially in diabetics, so if the drug is used for several days, blood glucose levels should be measured. When used in the treatment of toxemia, diazoxide may stop labor, because it relaxes uterine smooth muscle.

Veterinary Drugs and Treatments

Oral diazoxide is used in canine and ferret medicine for the treatment of hypoglycemia secondary to hyperinsulin secretion (e.g., insulinoma). Insulinomas are apparently very rare in the cat; there is little experience with this drug in that species.
In human medicine, intravenous diazoxide is sometimes used for treating severe hypertension.

代謝

Diazoxide lowers blood pressure within 3 to 5 minutes after rapid intravenous injection, and its duration of action may be 4 to 12 hours. Interestingly, if diazoxide is either injected slowly or infused its hypotensive action is quite modest.This is believed to be due to a rapid and extensive binding of the drug to plasma proteins. Both the liver and kidney contribute to its metabolism and excretion.The plasma half-life is therefore prolonged in patients with chronic renal failure.

ジアゾキシド 上流と下流の製品情報

原材料

準備製品


ジアゾキシド 生産企業

Global( 112)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21701 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29979 58
hdzhl biotechnology co., ltd
86-13032617415
sales@luchibiology.com CHINA 1029 58
Hebei Aicrowe Biotech Co., Ltd
0311-66855331
aicrowe@kf-chem.com CHINA 315 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 30864 58
Shanghai Synmedia Chemical Co., Ltd. +86 (21) 3868-1880
+86 (21) 3390-8196 sales@synmedia-chem.com China 158 58
Shanghai Elestone Pharmaceutical Technology Co., Ltd. 021-36680027/QQ:1762825045
sales@elestone.com.cn; sales2@elestone.com.cn China 296 58
hebei aicrowe co.,ltd 0311-66855331 15533616561
0311-66855331 parr-kf@hotmail.com China 12 58

364-98-7(ジアゾキシド)キーワード:


  • 364-98-7
  • DIAZOXIDE 364-98-7 kf-wang(at)kf-chem.com
  • Diazoxide API
  • DIAZOXIDE ACTIVATOR OF ATP-DEPE
  • Diazoxided
  • Eudemine
  • hyperstat
  • DIAZOXIDE,USP
  • NSC-64198
  • Sch-6783
  • 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
  • Diazoxide,7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
  • Diazoxide (200 mg)
  • 2h-1,2,4-benzothiadiazine,7-chloro-3-methyl-,1,1-dioxide
  • 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine1
  • 7-chloro-3-methyl-4h-1λ6,2,4-benzothiadiazine 1,1-dioxide
  • 7-cloro-3-metil-2h-1,2,4-benzotiodiazina-1,1-diossido
  • mutabase
  • proglicem
  • srg95213
  • 7-CHLORO-3-METHYL-2H-1,2,4-BENZOTHIADIAZINE 1,1-DIOXIDE
  • DIAZOXIDE
  • diazossido
  • dizoxide
  • 7-chloro-3-methyl-4H-1λ,2,4-benzothiadiazine-1,1-dione
  • ヒペルトナルム
  • プログリセム
  • 7-クロロ-3-メチル-2H-1,2,4-ベンゾチアジアジン1,1-ジオキシド
  • オイデミン
  • ジゾキシド
  • ジアゾキシド
  • ヒペルスタット
  • ムタベース
  • アログリセム
  • ジアゾキサイド
  • ジアゾキシド (JAN)
  • 降圧薬
  • 利尿薬
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