![ChemicalBook](https://m.chemicalbook.com/Scripts/New/img/logo.png)
![Аминоглутетимид структурированное изображение](/CAS/GIF/125-84-8.gif)
Аминоглутетимид
- английское имяAminoglutethimide
- CAS №125-84-8
- CBNumberCB5131691
- ФормулаC13H16N2O2
- мольный вес232.28
- EINECS204-756-4
- номер MDLMFCD00010122
- файл Mol125-84-8.mol
Температура плавления | 152-154 °C(lit.) |
Температура кипения | 374.44°C (rough estimate) |
плотность | 1.1099 (rough estimate) |
показатель преломления | 1.6450 (estimate) |
температура хранения | 2-8°C |
растворимость | H2O: 0.2 mg/mL, slightly soluble |
форма | Solid |
пка | 11.60±0.40(Predicted) |
цвет | white |
Растворимость в воде | Soluble in water (2 mg/ml at 20°C), methanol (50 mg/ml), ethanol (7 mg/ml at 25°C), DMSO (20 mg/ml at 25°C), and chloroform. |
Мерк | 14,440 |
Справочник по базе данных CAS | 125-84-8(CAS DataBase Reference) |
Рейтинг продуктов питания EWG | 1 |
Словарь онкологических терминов NCI | aminoglutethimide |
FDA UNII | 0O54ZQ14I9 |
Код УВД | L02BG01 |
Предложение 65 Список | Aminoglutethimide |
Справочник по химии NIST | Aminoglutethimide(125-84-8) |
Система регистрации веществ EPA | Aminoglutethimide (125-84-8) |
Коды опасности | Xi | |||||||||
Заявления о рисках | 36/37/38 | |||||||||
Заявления о безопасности | 26-36 | |||||||||
РИДАДР | 3249 | |||||||||
WGK Германия | 3 | |||||||||
RTECS | MA4026950 | |||||||||
Класс опасности | 6.1(b) | |||||||||
Группа упаковки | III | |||||||||
кода HS | 2925190100 | |||||||||
Банк данных об опасных веществах | 125-84-8(Hazardous Substances Data) | |||||||||
NFPA 704: |
|
рисовальное письмо(GHS)
-
рисовальное письмо(GHS)
-
сигнальный язык
предупреждение
-
вредная бумага
H315:При попадании на кожу вызывает раздражение.
H319:При попадании в глаза вызывает выраженное раздражение.
H335:Может вызывать раздражение верхних дыхательных путей.
-
оператор предупредительных мер
P261:Избегать вдыхания пыли/ дыма/ газа/ тумана/ паров/ аэрозолей.
P264:После работы тщательно вымыть кожу.
P271:Использовать только на открытом воздухе или в хорошо вентилируемом помещении.
P280:Использовать перчатки/ средства защиты глаз/ лица.
P302+P352:ПРИ ПОПАДАНИИ НА КОЖУ: Промыть большим количеством воды.
P305+P351+P338:ПРИ ПОПАДАНИИ В ГЛАЗА: Осторожно промыть глаза водой в течение нескольких минут. Снять контактные линзы, если Вы ими пользуетесь и если это легко сделать. Продолжить промывание глаз.
Аминоглутетимид химические свойства, назначение, производство
Описание
Aminoglutethimide is an aromatase inhibitor (IC50 = 7.5 μM). Aromatase inhibitors, including aminoglutethimide, inhibit estrogen synthesis via aromatase, suppressing estrogen levels in post-menopausal women. Formulations containing aromatase inhibitors have been used to treat estrogen receptor-positive breast cancer in post-menopausal women.Химические свойства
White SolidИспользование
Aminoglutethimide is used to decrease the production of sex hormones and suppress the growth of tumors that need sex hormones to grow. It blocks the production of steroids derived from cholesterol and is clinically used in the treatment of Cushing's syndrome and metastatic breast cancer. It is also a drug of abuse by body builders.Показания
Aminoglutethimide (Cytadren) is a competitive inhibitor of desmolase, the enzyme that catalyzes the conversion of cholesterol to pregnenolone; it also inhibits 11-hydroxylase activity.This drug also reduces estrogen production by inhibiting the aromatase enzyme complex in peripheral (skin, muscle, fat) and steroid target tissues.Определение
ChEBI: A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.Всемирная организация здравоохранения(ВОЗ)
Aminoglutethimide, a weak anticonvulsant, was introduced in 1960 for use in the treatment of epilepsy. However, its adrenocortical suppressant activity gave rise to serious adverse effects. The FDA decision in 1966 was taken in respect of a preparation indicated in epilepsy. In 1980 preparations containing aminoglutethimide were reintroduced in the USA exclusively for the treatment of Cushing's disease. In 1986 they were also registered in Saudi Arabia for use in Cushing's syndrome and for the treatment of breast cancer. In some other countries these preparations are additionally approved for carcinoma of the prostate.Общее описание
Aminoglutethimide, 3-(4-aminophenyl)-3-ethyl-2,6-piperidinedione, is mainly usedto treat Cushing syndrome, a condition of adrenal steroidexcess, a use in which the P450scc inhibition of thiscompound is exploited rather than its aromatase inhibition.Aminoglutethimide is a weak inhibitor of aromataseand has been used successfully in the treatment of estrogen-dependent breast cancer. Because of the developmentof more selective aromatase inhibitors, the use ofaminoglutethimide for its ability to inhibit aromatase is notsupported.Механизм действия
This drug blocks the transformation of cholesterol into pregnenolone, and androgens into estrogens in the adrenal glands, thus completely suppressing the production of all steroid hormones. Aminoglutethimide is used for palliative treatment of prostate carcinomas and post-menopausal breast carcinomas. Synonyms of aminoglutethimide are orimeten, citadren and others.Клиническое использование
Aminoglutethimide is suitable for use in Cushing’s syndrome that results from adrenal carcinoma and in congenital adrenal hyperplasia, in which it protects the patient from excessive secretion of endogenous androgens. The drug is not curative, and relapse occurs when treatment is terminated. Since aminoglutethimide therapy is frequently associated with mineralocorticoid deficiency, mineralocorticoid supplements may be needed. Aminoglutethimide and metyrapone are frequently used in combination at lower doses of both drugs as an adjunct to radiation or surgical therapy.Побочные эффекты
Such a medical adrenalectomy is an efficacious treatment for metastatic breast and prostate cancer, since it diminishes the levels of circulating sex hormones. Glucocorticoids are administered concomitantly to suppress enhanced corticotrophin release. Cortisol is preferable to dexamethasone in this situation because aminoglutethimide markedly enhances the hepatic microsomal metabolism of dexamethasone. Hepatic enzyme induction may be responsible for the development of tolerance to the side effects of aminoglutethimide, such as ataxia, lethargy, dizziness, and rashes.Метаболический путь
Following administration of a single oral dose of 14C- aminoglutethimide to rats, guinea pigs, rabbits, and man, more than 89% of the dose is excreted in urine and feces within 72h, and dogs eliminate only 51% in this time. Extensive metabolism occurs in all species, with N-acetylaminoglutethimide being the major metabolite except for dogs and man. In the latter two species, the unchanged drug is the main product excreted. As shown in the pathways, it appears that aminoglutethimide is metabolized by several pathways in man and, of the ten metabolites, only two are present in any quantity, namely N-acetylaminoglutethimide and N-hydroxyaminoglutethimide, the latter increasing during the course of treatment.Аминоглутетимид запасные части и сырье
Аминоглутетимид поставщик
поставщик | телефон | страна | номенклатура продукции | благоприятные условия |
---|---|---|---|---|
+86-0371-55170693 +86-19937530512 |
China | 21667 | 55 | |
+86-0371-86658258 +8613203830695 |
China | 29889 | 58 | |
+86-755-89396905 +86-15013857715 |
China | 10312 | 58 | |
86-13657291602 | CHINA | 22968 | 58 | |
0086-182-6772-3597 | CHINA | 419 | 58 | |
+86-023-6139-8061 +86-86-13650506873 |
China | 39916 | 58 | |
+8618523575427 | China | 49392 | 58 | |
+1-781-999-5354 +1-00000000000 |
United States | 19892 | 58 | |
+86-0551-65418671 +8618949823763 |
China | 34571 | 58 | |
86-571-88216897,88216896 13588875226 |
CHINA | 6313 | 58 |