Limaprost is an analog of PGE1 with structural modifications intended to give a prolonged half-life and greater potency. It is orally active in both guinea pigs and rats at doses of 100 μg/kg as an inhibitor of ADP and collagen induced platelet aggregation. Je 10-1,000 times more potent than PGE1 as a platelet adhesive inhibitor, measured in vitro. Intra-coronary injection (100 ng/kg) or intravenous injection (3 μg/kg) in anesthetized dogs causes vasodilation and increased coronary blood flow by 60-80%. Significant hypotensive effects were seen at 100 in 300 μg/kg orally in rats.
Limaprost (as Limaprost alfadex; številka CAS 88852-12-4) is an oral prostaglandin E1 analog. Prostaglandins act on a variety of cells such as vascular smooth muscle cells causing constriction or dilation, on platelets causing aggregation or disaggregation and on spinal neurons causing pain. Prostaglandins have a wide variety of actions, vključno z, but not limited to muscular constriction and mediation of inflammation. Limaprost alfadex has been shown to improve peripheral circulatory failure with a vasodilator action and an antithrombotic effect. It also improves poor blood flow in the nerve tissue in cervical spondylosis and normalizes nerve function. Limaprost alfadex was discovered from collaborative research between Ono Pharmaceutical (Ono) and Dainippon Sumitomo Pharma (DSP). It was approved for the treatment of ischemic symptoms such as skin ulcer, pain and coldness accompanying thromboangiitis obliterans in 1988; in za zdravljenje subjektivnih simptomov, kot so bolečina in otrplost v spodnjem delu noge ter motnje hoje, povezane s pridobljeno stenozo ledvenega hrbteničnega kanala, kot dodatna indikacija pri 2001. Zdravilo se prodaja pod trgovskim imenom Opalmon® Tablets podjetja Ono in Prorenal® Tablets podjetja DSP.. notri 2011, Ono in DSP sta na Japonskem začela klinična preskušanja druge faze za zdravljenje sindroma karpalnega kanala. notri 2013, ta preskušanja so prekinili, ker študija ni dokazala učinkovitosti. Ono in DSP sta tudi prekinila razvoj limaprosta alfadexa za dodatno indikacijo cervikalne spondiloze v 2008 zaradi neuspeha dokaza pričakovane učinkovitosti v študiji faze II pri bolnikih s to boleznijo. Vendar, to je novembra potrdila Nacionalna univerzitetna bolnišnica v Seulu 2014 da študija o učinkovitosti peroralnega limaprosta alfadexa po operaciji cervikalne mielopatije še poteka.
