Pioglitazone Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R11:Leichtentzündlich.
R34:Verursacht Verätzungen.
S-Sätze Betriebsanweisung:
S16:Von Zündquellen fernhalten - Nicht rauchen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
Pioglitazone is an agonist of the peroxisome proliferator-activated receptor γ (PPARγ; EC
50 = ~500-600 nM for both human and murine PPARγ). It is selective for PPARγ over PPARα, exhibiting low level activation of PPARα at 1 μM and 5.4-fold activation at a concentration of 10 μM. Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 μM.
In vivo, pioglitazone (0.3-3 mg/kg per day) reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats. It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model. Pioglitazone (2.5 mg/kg) also decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress, indicating antidepressant-like activity that can be reversed by the PPARγ antagonist GW9662 .
Verwenden
Pioglitazone shows antidiabetic activity in patients with type 2 diabetes mellitus.
Indications
Pioglitazone is approved for use as monotherapy
and in conjunction with metformin, sulfonylureas, and
insulin. It is taken once a day with or without food.
Though pioglitazone may also cause a small increase in
low-density lipoprotein concentrations, there is usually
a modest decrease in triglyceride levels, but it unclear
whether this has any clinical significance or persists in
the long term.
Definition
ChEBI: A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic acti
ity.
Allgemeine Beschreibung
Pioglitazone, (±)-5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione (Actos),is an odorless, white, crystalline powder that must be convertedto a salt such as its hydrochloride before it will haveany water solubility. Although the molecule contains one chiralcenter, the compound is used as the racemic mixture. Thisis primarily a result of the in vivo interconversion of the twoenantiomers. Thus, there are no differences in the pharmacologicalactivity of the two enantiomers.
Pioglitazone Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
