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Metyrapon

METYRAPONE Struktur
54-36-4
CAS-Nr.
54-36-4
Bezeichnung:
Metyrapon
Englisch Name:
METYRAPONE
Synonyma:
Metapyron;Metopirone;su4885;Su 4885;su-4885;Metopiron;Metyrapon;NSC-25265;ETYRAPONE;Metapyrone
CBNumber:
CB8329426
Summenformel:
C14H14N2O
Molgewicht:
226.27
MOL-Datei:
54-36-4.mol

Metyrapon Eigenschaften

Schmelzpunkt:
52-55 °C(lit.)
Siedepunkt:
367.89°C (rough estimate)
Dichte
1.0852 (rough estimate)
Brechungsindex
1.6419 (estimate)
Flammpunkt:
>230 °F
storage temp. 
Inert atmosphere,Room Temperature
L?slichkeit
H2O: soluble (sparingly)
Aggregatzustand
solid
pka
4.61±0.10(Predicted)
Farbe
White
Merck 
13,6181
BRN 
163023
Stabilit?t:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
EPA chemische Informationen
Metyrapone (54-36-4)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher Xn
R-S?tze: 22-36/37/38
S-S?tze: 26
WGK Germany  3
RTECS-Nr. UC3050000
HS Code  2933399090
Giftige Stoffe Daten 54-36-4(Hazardous Substances Data)
Toxizit?t A well-known inhibitor of monooxygenase reactions and can also, under some circumstances, stimulate metabolism of xenobiotics in vitro. In either case, the effect is non-competitive, in that the KM does not change whereas Vmax does, decreasing in the case of inhibition and increasing in the case of stimulation.
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P270 Bei Gebrauch nicht essen, trinken oder rauchen.
P301+P312 BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.
P302+P352 BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

Metyrapon Chemische Eigenschaften,Einsatz,Produktion Methoden

R-S?tze Betriebsanweisung:

R22:Gesundheitssch?dlich beim Verschlucken.
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.

Verwenden

Metyrapone acts as a glucocorticoid synthesis inhibitor, maintaining stress-hormone levels.

Biologische Aktivit?t

Cytochrome P450 inhibitor. Blocks glucocorticoid synthesis via inhibition of steroid 11- β hydroxylase (CYP11B1) activity (IC 50 = 7.83 μ M). Also inhibits CYP3A4 and cytochrome P450-mediated ω / ω -1 hydroxylase activity.

Mechanism of action

Metyrapone (Metopirone) produces its primary pharmacological effect by inhibiting 11-β-hydroxylase, thereby causing diminished production and release of cortisol. The resulting reduction in the negative feedback of cortisol on the hypothalamus and pituitary causes an increase in corticotrophin release and in the secretion of precursor 11-deoxysteroids.

Clinical Use

Metyrapone is used in the differential diagnosis of both adrenocortical insufficiency and Cushing’s syndrome (hypercortisolism). The drug tests the functional competence of the hypothalamic–pituitary axis when the adrenals are able to respond to corticotrophin; that is, when primary adrenal insufficiency has been ruled out.
After metyrapone administration, a patient with a disease of pituitary origin cannot achieve a compensatory increase in the urinary excretion of 17-hydroxycorticosteroids or 11-deoxysteroids. Moreover, if pituitary corticotrophin is suppressed by an autonomously secreting adrenal carcinoma, there will be no increase in response to metyrapone. On the other hand, if pituitary corticotrophin secretion is maintained, as occurs in adrenal hyperplasia, the inhibition of corticoid synthesis produced by metyrapone will stimulate corticotrophin secretion and the release of metabolites of precursor urinary steroids, which can be measured as 17-hydroxycorticosteroids. Metyrapone is now used less frequently in the differential diagnosis of Cushing’s syndrome because of the ability to measure plasma corticotrophin directly.
The steroid-inhibiting properties of metyrapone have also been used in the treatment of Cushing’s syndrome, and it remains one of the more effective drugs used to treat this syndrome. However, the compensatory rise in corticotrophin levels in response to falling cortisol levels tends to maintain adrenal activity.This requires that glucocorticoids be administered concomitantly to suppress hypothalamic–pituitary activity. Although metyrapone interferes with 11β- and 18- hydroxylation reactions and thereby inhibits aldosterone synthesis, it may not cause mineralocorticoid deficiency because of the compensatory increased production of 11-desoxycorticosterone.

Nebenwirkungen

Side effects associated with the use of metyrapone include gastrointestinal distress, dizziness, headache, sedation, and allergic rash. The drug should not be used in cases of adrenocortical insufficiency or when hypersensitivity reactions can be expected. When administered to pregnant women during the second or third trimesters, the drug may impair steroid biosynthesis in the fetus. Because metyrapone is relatively nontoxic, it is used in combination therapy with the more toxic aminoglutethimide to reduce its dosage.

Metyrapon Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Metyrapon Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 124)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 58
SHANDONG ZHI SHANG CHEMICAL CO.LTD
+86 18953170293
sales@sdzschem.com China 2930 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63687 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
Shaanxi Dideu Medichem Co. Ltd
+86-029-89586680 +86-18192503167
1026@dideu.com China 7724 58
AFINE CHEMICALS LIMITED
+86-0571-85134551
sales@afinechem.com China 15352 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471
sales@sarms4muscle.com China 10473 58

54-36-4(Metyrapon)Verwandte Suche:


  • Metapirone
  • Metapyrone
  • Methapyrapone
  • Methbipyranone
  • Methopirapone
  • Methopyrapone
  • Methopyrinine
  • Methopyrone
  • Metopiron
  • Metopyrone
  • Metroprione
  • Metyrapon
  • Su 4885
  • su4885
  • su-4885
  • 1-methyl-1-(3-pyridyl)ethyl 3-pyridyl ketone
  • 1,2-di-3-pyridyl-2-methyl-1-propanon
  • 1,2-di-3-pyridyl-2-methyl-1-propanone
  • 1-Propanone, 2-methyl-1,2-di-3-pyridinyl-
  • 1-Propanone, 2-methyl-1,2-di-3-pyridyl-
  • 1-propanone,2-methyl-1,2-di-3-pyridinyl
  • 2-methyl-1,2-bis(3-pyridyl)-1-propane
  • 2-methyl-1,2-bis(3-pyridyl)-1-propanone
  • 2-Methyl-1,2-di(3-pyridinyl)-1-propanone
  • 2-methyl-1,2-di-3-pyridinyl-1-propanon
  • 2-methyl-1,2-di-3-pyridinyl-1-propanone
  • 2-methyl-1,2-di-3-pyridyl-1-propanon
  • 2-Methyl-1,3-di-3-pyridiyl-1-propanone
  • Mepyrapone
  • 2-methyl-1,2-bis(3-pyridyl)propan-1-one
  • 2-methyl-1,2-di(pyridin-3-yl)propan-1-one
  • 2-Methyl-1,2-di-3-pyridyl-1-propanone,Metyrapone, Su-4885
  • Metyrapone (200 mg)
  • Metyrapone USP
  • 2-METHYL-1,2-DI-3-PYRIDYL-1-PROPANE
  • Metyrapone, Su-4885
  • METYRAPONE
  • 2-METHYL-1,2-DI(3-PYRIDYL)-1-PROPANONE
  • Metyrapone (1443001)
  • METYRAPONE USP/EP/BP
  • 2-methyl-1, 2-?di-3-pyx idyl-l-propanone
  • NSC-25265
  • Metopirone
  • Metapyron
  • 3-Methyl-1,2-di-3-pyridyl-1-propanone
  • ETYRAPONE
  • 54-36-4
  • C9 to C46
  • Building Blocks
  • Heterocyclic Building Blocks
  • Pyridines
  • Cytochrome P450 isozyme
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