Aminoglutethimid
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Aminoglutethimid Eigenschaften
- Schmelzpunkt:
- 152-154 °C(lit.)
- Siedepunkt:
- 374.44°C (rough estimate)
- Dichte
- 1.1099 (rough estimate)
- Brechungsindex
- 1.6450 (estimate)
- storage temp.
- 2-8°C
- L?slichkeit
- H2O: 0.2 mg/mL, slightly soluble
- pka
- 11.60±0.40(Predicted)
- Aggregatzustand
- Solid
- Farbe
- white
- Wasserl?slichkeit
- 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.
- Merck
- 14,440
- CAS Datenbank
- 125-84-8(CAS DataBase Reference)
- NIST chemische Informationen
- Aminoglutethimide(125-84-8)
- EPA chemische Informationen
- Aminoglutethimide (125-84-8)
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher | Xi | ||
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R-S?tze: | 36/37/38 | ||
S-S?tze: | 26-36 | ||
RIDADR | 3249 | ||
WGK Germany | 3 | ||
RTECS-Nr. | MA4026950 | ||
HazardClass | 6.1(b) | ||
PackingGroup | III | ||
HS Code | 2925190100 | ||
Giftige Stoffe Daten | 125-84-8(Hazardous Substances Data) |
Bildanzeige (GHS) | |||||||||||||||||||||||||||||
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Sicherheit |
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Aminoglutethimid Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.S-S?tze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.Chemische Eigenschaften
White SolidVerwenden
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.Indications
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.Definition
ChEBI: A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.Weltgesundheitsorganisation (WHO)
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.Allgemeine Beschreibung
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.Mechanism of action
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.Clinical Use
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.Nebenwirkungen
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.Stoffwechselwegen
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.Aminoglutethimid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Salpetersure
Wasserstoff
3-Ethyl-3-(4-nitrophenyl)piperidin-2,6-dion
2-Ethyl-2-phenylglutaronitril
ethyl 2-(4-nitrophenyl)butanoate
DL-2-Phenylbutyronitril
Nitrobenzol
Phenylacetonitril
Downstream Produkte
Aminoglutethimid Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 171)Lieferanten
Firmenname | Telefon | Land | Produktkatalog | Edge Rate | |
---|---|---|---|---|---|
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21634 | 55 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29880 | 58 |
Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 |
admin@nexconn.com | China | 10311 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 |
linda@hubeijusheng.com | CHINA | 22963 | 58 |
Beijing Yibai Biotechnology Co., Ltd | 0086-182-6772-3597 |
sales04@yibaibiotech.com | CHINA | 419 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 |
sales@chemdad.com | China | 39894 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 49374 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 |
marketing@targetmol.com | United States | 32161 | 58 |
Hefei TNJ Chemical Industry Co.,Ltd. | +86-0551-65418671 +8618949823763 |
sales@tnjchem.com | China | 34563 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 |
sales@hzclap.com | CHINA | 6312 | 58 |
125-84-8(Aminoglutethimid)Verwandte Suche:
Ethylenglykolmonoethylether
Ethanol
Ethylpropionat
ISOXADIFEN-ETHYL
Ethylacetat
4,4'-Piperidindiol, hydrochlorid
Trinexapac-ethyl
Ameisens?ure-ethylester
3-Aminoacetophenon
Ethyl-4-hydroxybenzoat
2-Piperidon
3,4'-DIAMINODIPHENYLMETHANE
Diethylether
Glutarimid
Butanon
3-Ethyl-3-phenyl-2,6-piperidindion
Aminoglutethimid
- TIMTEC-BB SBB000711
- 2-(4-aminophenyl)-2-ethylglutarimide
- DL-Aminoglutethimide 99 %
- (+/-)-P-AMINOGLUTETHIMIDE INHIBITS CYTOC HROME P
- Aminoglutethimide(Ag)
- 2-(p-aminophenyl)-2-ethyl-glutarimid
- 2-(p-Aminophenyl)-2-ethylglutarimide
- 2-(p-Aminophenyl)-2-ethylglutarimide2,6-piperidinedione, 3-(4-aminophenyl)-3-ethyl-
- 2,6-Piperidinedione, 3-(4-aminophenyl)-3-ethyl-
- 3-(4-aminophenyl)-3-ethyl-6-piperidinedione
- 3-Ethyl-3-(p-aminophenyl)-2,6-dioxopiperidine
- alpha-(p-Aminophenyl)-alpha-ethylglutarimide
- Ba-16038
- Elipten
- Glutarimide, 2-(p-aminophenyl)-2-ethyl-
- NSC-330915
- 3-(4-AMINOPHENYL)-3-ETHYL-2,6-PIPERIDINEDIONE (DL-AMINOGLUTETHIMIDE)
- (S)-3-(4-Aminophenyl)-3-ethyl-2,6-piperidinedione
- 3-(4-aminophenyl)-3-ethyl-piperidine-2,6-quinone
- 3-(4-azanylphenyl)-3-ethyl-piperidine-2,6-dione
- DL-Aminoglutethimide,3-(4-Aminophenyl)-3-ethyl-2,6-piperidinedione, 3-(p-Aminophenyl)-3-ethylpiperidine-2,6-dione
- Aminoglutethimide (200 mg)
- (RS)-2-(4-AMino-phenyl)-2-ethyl-glutariMide, (RS)-3-(4-AMino-phenyl)-3-ethyl-2,6-dioxo-piperidine
- 3-(4-AMINOPHENYL)-3-ETHYL-2,6-PIPERIDINEDIONE
- AKOS NCG1-0032
- AMINOGLUTETHIMIDE
- 3-[P-AMINOPHENYL]-3-ETHYLPIPER-IDINE-2,6-DIONE
- (RS)-2-ETHYL-2-(4-AMINO-PHENYL)-GLUTARIMIDE
- (RS)-3-(4-AMINO-PHENYL)-3-ETHYL-PIPERIDINE-2,6-DIONE
- (RS)-3-ETHYL-3-(4-AMINO-PHENYL)-2,6-DIOXO-PIPERIDINE
- (+/-)-P-AMINOGLUTETHIMIDE
- ORIMETEN
- DL-3-(4-AMINOPHENYL)-3-ETHYL-2,6-PIPERIDINEDIONE
- Aminoglutethimide CRS
- Aminoglutethimide USP/EP/BP
- Aminoglutethimide (BA-16038)
- Aminoglutethimide 98% (HPLC)
- Aminoglutethimide (1025205)
- Cytadren
- AMINOGLUTETHAMIDE
- 3-(4-AMINOPHENYL)-3-ETHYLPIPERIDINE-2,6-DIONE
- DL-AMINOGLUTETHIMIDE
- Venlafaxine Impurity 32
- 125-84-8
- 125-84-4
- C13H16N2O2
- Cell Biology
- Cell Signaling and Neuroscience
- BioChemical
- Cytokines, Growth Factors and Hormones
- Hormones
- Steroid Hormones
- Other Steroid Products
- CYTADREN
- Antitumors for Research and Experimental Use
- Biochemistry
- Inhibitors
- Intermediates & Fine Chemicals