Iloprost-d4

Iloprost-d4 is a labelled 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.

[1] MARK ABRAMOVITZ . The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 2000, 1483 2: Pages 285-293. DOI: 10.1016/s1388-1981(99)00164-x
[2] BRENDAN J. WHITTLE . Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: Treprostinil is a potent DP1 and EP2 agonist[J]. Biochemical pharmacology, 2012, 84 1: Pages 68-75. DOI: 10.1016/j.bcp.2012.03.012
[3] K SCHRÖR. The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK 36 374)–equipotent to PGI2 in vitro.[J]. Naunyn-Schmiedeberg’s archives of pharmacology, 1981, 316 3: 252-255. DOI: 10.1007/bf00505658
[4] WILLEM J VAN DER GIESSEN . The effect of the stable prostacyclin analogue ZK 36374 on experimental coronary thrombosis in the pig[J]. Thrombosis research, 1984, 36 1: Pages 45-51. DOI: 10.1016/0049-3848(84)90375-x
[5] RALPH THEO SCHERMULY. Inhaled iloprost reverses vascular remodeling in chronic experimental pulmonary hypertension.[J]. American journal of respiratory and critical care medicine, 2005, 172 3: 358-363. DOI: 10.1164/rccm.200502-296oc