Limaprost

• CAT Number: I004763
• CAS Number: 74397-12-9
• Molecular Formula: C22H36O5
• Molecular Weight: 380.5
• Purity: ≥95%
• Target: Others
• Solubility: DMSO:40mg/mL
• Storage: -20°C
• InChIKey: OJZYRQPMEIEQFC-UAWLTFRCSA-N

Limaprost(OP1206) is a PGE1 analog and potent platelet adhesion inhibitor.Target: OthersLimaprost, an alprostadil (prostaglandin E1) analogue, is a vasodilator that increases blood flow and inhibits platelet aggregation. Limaprost is a n 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 g/kg as an inhibitor of ADP and collagen induced platelet aggregation. It is 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 g/kg) in anesthetized dogs causes vasodilation and increased coronary blood flow by 60-80%. Significant hypotensive effects were seen at 100 and 300 g/kg orally in rats [1].

Reference

1:Ternary inclusion complex formation and stabilization of limaprost, a prostaglandin E1 derivative, in the presence of α- and β-cyclodextrins in the solid state. Inoue Y, Iohara D, Sekiya N, Yamamoto M, Ishida H, Sakiyama Y, Hirayama F, Arima H, Uekama K.Int J Pharm. 2016 Jul 25;509(1-2):338-47. doi: 10.1016/j.ijpharm.2016.06.018. Epub 2016 Jun 7. PMID: 27286633 2:Lichenoid Drug Eruption Caused by Limaprost Alfadex. Inoue A, Sawada Y, Ohmori S, Omoto D, Haruyama S, Yoshioka M, Nishio D, Nakamura M.Acta Derm Venereol. 2016 Nov 2;96(7):997-998. doi: 10.2340/00015555-2435. No abstract available. PMID: 27068583 Free Article3:Comparative study of the efficacy of limaprost and pregabalin as single agents and in combination for the treatment of lumbar spinal stenosis: a prospective, double-blind, randomized controlled non-inferiority trial. Kim HJ, Kim JH, Park YS, Suk KS, Lee JH, Park MS, Moon SH.Spine J. 2016 Jun;16(6):756-63. doi: 10.1016/j.spinee.2016.02.049. Epub 2016 Mar 29. PMID: 27045252 4:Formation of the ternary inclusion complex of limaprost with α- and β-cyclodextrins in aqueous solution. Inoue Y, Sekiya N, Yamamoto M, Iohara D, Hirayama F, Uekama K.Chem Pharm Bull (Tokyo). 2015;63(5):318-25. doi: 10.1248/cpb.c14-00733. PMID: 25948325 Free Article5:Single- and multiple-dose pharmacokinetics and tolerability of limaprost in healthy Chinese subjects. Chen H, Zhang Q, Li X, Zhang H, Sun Y, Yin L, Liu C, Cao Y, Gu J, Ding Y.Clin Drug Investig. 2015 Mar;35(3):151-7. doi: 10.1007/s40261-014-0265-3. PMID: 25586152 6:Comparisons on efficacy of elcatonin and limaprost alfadex in patients with lumbar spinal stenosis and concurrent osteoporosis: a preliminary study using a crossover design. Kanchiku T, Imajo Y, Suzuki H, Yoshida Y, Taguchi T, Tominaga T, Toyoda K.Asian Spine J. 2014 Aug;8(4):469-75. doi: 10.4184/asj.2014.8.4.469. Epub 2014 Aug 19. PMID: 25187864 Free PMC Article7:Stabilizing effect of β-cyclodextrin on Limaprost, a PGE₁ derivative, in Limaprost alfadex tablets (Opalmon) in highly humid conditions. Inoue Y, Sekiya N, Katayama K, Narutaki S, Yamamoto M, Iohara D, Hirayama F, Uekama K.Chem Pharm Bull (Tokyo). 2014;62(8):786-92. Epub 2014 May 23. PMID: 24859193 Free Article8:Plasmapheresis-refractory transplantation-associated thrombotic microangiopathy successfully treated with pravastatin and limaprost alfadex. Uesawa M, Muroi K, Ozawa K.Ther Apher Dial. 2013 Aug;17(4):462-3. doi: 10.1111/1744-9987.12015. Epub 2013 Feb 17. No abstract available. PMID: 23931890 9:Limaprost alfadex and nonsteroidal anti-inflammatory drugs for sciatica due to lumbar spinal stenosis. Onda A, Kikuchi S, Yabuki S, Otani K, Nikaido T, Watanabe K, Konno S.Eur Spine J. 2013 Apr;22(4):794-801. doi: 10.1007/s00586-012-2551-1. Epub 2012 Oct 23. PMID: 23090093 Free PMC Article10:Limaprost alfadex, a prostaglandin E1 derivative, prevents deterioration of forced exercise capability in rats with chronic compression of the spinal cord. Kurokawa R, Nagayama E, Murata H, Kim P.Spine (Phila Pa 1976). 2011 May 15;36(11):865-9. doi: 10.1097/BRS.0b013e3181e878a1. PMID: 21192291