ILOPROST Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Iloprost is a stable epoprostenol derivative which acts as an inhibitor of platelet
aggregation and is recommended for the treatment of peripheral vascular diseases. The
compound was shown to be a potent agonist at PGE
2-sensitive and
prostacyclin-sensitive receptors in animal studies. Iloprost is administered by IV
infusion and has been reported to have beneficial effects in Buerger's and Raynaud's
diseases as well as peripheral artery occlusive disease.
Chemische Eigenschaften
Colourless Oil
Verwenden
A synthetic analogue of Prostacyclin (PGI2) used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon and ischemia. It acts through elevation of cAMP by binding to the prostacyclin receptor (IP receptor). Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time.
Definition
ChEBI: A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R
/stereo>)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension.
Health Hazard
Exposures to quinine vapor are highly irritating to the eyes and may be followed by corneal
opacities, structural changes in the cornea, and loss of vision. Solid quinone may
produce discoloration, severe irritation, swelling, and form papules and vesicles.
Biologische Aktivität
Prostacyclin (PGI 2 ) analog that binds with high affinity to IP, EP 1 and EP 3 receptors (K i values are 11, 11, 56, 284, 619, 1035, 1870 and 6487 nM for IP, EP 1 , EP 3 , EP 4 , FP, DP, EP 2 and TP receptors respectively). Inhibits platelet aggregation induced by collagen, thrombin and ADP (IC 50 values are 0.24, 0.71 and 1.07 nM respectively).
ILOPROST Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
