Cicaprost (ZK 96480) is a prostacyclin receptor (IP) agonist, which induces relaxation of the artery via concentration-dependent mechanisms. Its EC50 value, determined to be 5.8 nM [1], further highlights its potency.

Cicaprost significantly reduces proliferation of human pulmonary artery smooth muscle cells (HPASMC) stimulated by fetal bovine serum (FBS). Cicaprost displays marked antiproliferative activity at 30 nM [2]. Cicaprost stimulates [ 3 H]cyclic AMP production with EC 50 values of 1.5-22 nM, and stimulates [ 3 H]inositol phosphate production (EC 50 values 49-457 nM) in all but the SK-N-SH cells [3]. Cell Proliferation Assay [2] Cell Line: HPASMC Concentration: 10 pM, 100 pM, 1 nM, 10 nM, 100 nM, 1 μM, and 10 μM Incubation Time: Result: Dose-dependently inhibited proliferation with an EC 50 of 24.1 nM.

Cicaprost alters pain perception and inflammatory response in mice lacking prostacyclin receptor. Intravenous injection of Cicaprost (1 μg/kg) causes hypotension of ～30 mm Hg in anaesthetized wild-type mice [4]. Animal Model: Wild-type (+/+) and IP / mice [4] Dosage: 1 μg/kg Administration: Intravenous injection Result: Caused hypotension of ～30 mm Hg in anaesthetized wild-type mice, whereas there was no change in blood pressure in IP-deficient mice even at 10 μg/kg.