Alprostadil is an analog of prostaglandin which is prostaglandin E1 agonist with vasodilatory properties and can be used to treat erectile dysfunction.
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Prostaglandin E1 (Alprostadil) is a ligand for prostanoid receptors, exhibiting Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM, and 36 nM for mouse EP3, EP4, EP2, IP, and EP1 receptors respectively. It induces vasodilation and inhibits platelet aggregation, being researched as a vasodilator for peripheral vascular diseases[1].[2].[3].
体内研究
Subcutaneously administered at 20 ng/animal/day for four days, it significantly inhibits FGF-induced angiogenesis in mice[2].
体外研究
In experiments, Prostaglandin E1 at concentrations ranging from 1 nM to 10 μM over 48 hours, reduces proliferation of HUVECs (up to 100% inhibition) in the presence of VEGF (20 ng/mL) with an IC50 of 400 nM[2].
Prostaglandin E1 also inhibits VEGF-induced HUVECs migration at doses from 0.01 μM to 10 μM over 6 hours, with an IC50 of 500 nM[2], and restricts in vitro angiogenesis at 1-5 μM over 12-18 hours[2].
Additionally, Prostaglandin E1 increases intracellular cAMP levels in HUVECs within 20 minutes when administered at concentrations from 0.01 μM to 10 μM[2].
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