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Limaprost Sale

(Synonyms: 利马前列素; 17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206) 目录号 : GC36463

A stable, potent analog of PGE1

Limaprost Chemical Structure

Cas No.:74397-12-9

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10mM (in 1mL DMSO)
¥1,794.00
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2mg
¥1,080.00
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5mg
¥2,143.00
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10mg
¥3,809.00
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50mg
¥16,699.00
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产品描述

Limaprost is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency. Limaprost is orally active in both rats and guinea pigs at doses of 100 ?g/kg as an inhibitor of ADP and collagen induced platelet aggregation. Limaprost is 10-1,000 times more potent than PGE1 as an inhibitor of platelet adhesiveness 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

1.Tsuboi, T., Hatano, N., Nakatsuji, K., et al.Pharmacological evaluation of OP 1206, a prostaglandin E1 derivative, as an antianginal agentArch. Int. Pharmacodyn. Ther.247(1)89-102(1980)

Chemical Properties

Cas No. 74397-12-9 SDF
别名 利马前列素; 17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206
Canonical SMILES O=C(O)/C=C/CCCC[C@@H]1[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)CC1=O
分子式 C22H36O5 分子量 380.52
溶解度 DMSO: ≥ 40 mg/mL (105.12 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.628 mL 13.1399 mL 26.2798 mL
5 mM 0.5256 mL 2.628 mL 5.256 mL
10 mM 0.2628 mL 1.314 mL 2.628 mL
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Research Update

Limaprost

Drugs 2007;67(1):109-18; discussion 119-20.PMID:17209669DOI:10.2165/00003495-200767010-00010.

Limaprost, an alprostadil (prostaglandin E1) analogue, is a vasodilator that increases blood flow and inhibits platelet aggregation. The efficacy of oral Limaprost was evaluated in adult Japanese patients in three randomised, double-blind, 6-week trials. One study included patients with thromboangiitis obliterans and two trials included patients with lumbar spinal canal stenosis. Limaprost was generally well tolerated and serious adverse events were uncommon. THROMBOANGIITIS OBLITERANS: In a randomised, double-blind trial in Japanese patients primarily with thromboangiitis obliterans (n=136), there was no significant difference between patients receiving Limaprost 30 microg/day and those receiving oral ticlopidine 500 microg/day in the improvement of ischaemic symptoms. LUMBAR SPINAL CANAL STENOSIS: Limaprost 15 microg/day was superior to Limaprost 3 microg/day for overall drug usefulness and overall improvement from baseline to study end in a phase III trial in 146 patients with lumbar spinal canal stenosis. Assessment of overall improvement considered various objective symptoms (e.g. muscle strength, walking ability) and subjective symptoms (e.g. pain or numbness in extremities), while overall usefulness also considered safety issues. The efficacy of Limaprost 15 microg/day was not significantly different from that of 30 microg/day, but tended to be better than that of 6 microg/day in a phase II trial in patients with lumbar spinal canal stenosis and normal straight leg raise test results. The optimal dosage of Limaprost for this indication was therefore deemed to be 15 microg/day.

Limaprost or Pregabalin: Preoperative and Postoperative Medication for Pain due to Lumbar Spinal Stenosis

Pain Pract 2018 Jun;18(5):625-630.PMID:29080243DOI:10.1111/papr.12653.

Purpose: We aimed to evaluate the incidence of (and risk factors for) postoperative pregabalin and/or Limaprost to treat persistent numbness and/or pain of the lower extremities after lumbar spinal stenosis (LSS) surgery. Methods: Medical records of 329 patients (168 men, 161 women; average age 70 years) were retrospectively reviewed for data on the duration of LSS diagnosis; LSS disease; preoperative medication (Limaprost, pregabalin, or combined Limaprost/pregabalin; duration); symptoms; preoperative/postoperative intermittent claudication (IC); operation type; and postoperative medication and period. Results: Limaprost, pregabalin, and combined Limaprost/pregabalin were prescribed preoperatively for 43%, 7%, and 5% of patients, respectively. At an average of 21 months postoperatively, Limaprost, pregabalin, and combined therapy were prescribed in 11%, 8%, 4% of patients, respectively. Medication requirement was significantly lower postoperatively than preoperatively (P < 0.0001). Significant risk factors for required postoperative medication were required preoperative medication (odds ratio [OR] 3.088, 95% confidence interval [CI] 1.679 to 5.681]; postoperative period (OR 1.063, 95% CI 1.031 to 1.096); and postoperative IC (OR 3.868, 95% CI 1.481 to 10.103). A negative impact from postoperative medication was seen in patients who had undergone decompression surgery (OR 0.589, 95% CI 0.377 to 0.918). Conclusions: Overall, 23% of LSS patients required medication for pain and/or numbness at 21 months postoperatively. Significant factors portending required postoperative medication were preoperative medication, longer postoperative period, and postoperative IC. A negative influence from postoperative medication was seen in patients who had undergone decompression surgery without fusion.

Limaprost alfadex and nonsteroidal anti-inflammatory drugs for sciatica due to lumbar spinal stenosis

Eur Spine J 2013 Apr;22(4):794-801.PMID:23090093DOI:10.1007/s00586-012-2551-1.

Purpose: Limaprost, a prostaglandin E1 analog, has vasodilatory properties and increases blood flow of the nerve root. However, it has not been clarified whether Limaprost affects pain sensation associated with radiculopathy due to lumbar spinal stenosis (LSS). The aim of this study was to compare the efficacy of oral Limaprost with nonsteroidal anti-inflammatory drugs (NSAIDs) for radiculopathy. Methods: We performed a multicenter prospective randomized trial. Patients with LSS who had radicular-type neurologic intermittent claudication assessed based on a self-reported diagnostic support tool were randomized into three treatment groups. Limaprost, NSAIDs, or Limaprost plus NSAIDs were administered orally for 6 weeks. Leg pain, low back pain (LBP) and the associated symptoms were assessed by a numerical rating scale (NRS) both at rest and on movement as well as the Roland-Morris Disability Questionnaire (RDQ) and Short Form (SF)-36. Results: Sixty-one patients were enrolled in the study. Each treatment finally reduced radicular pain, and the improvement was prominent in a combination treatment. There were no significant differences in radicular pain among three groups at final follow-up. LBP was not influenced by Limaprost, and a significant reduction of LBP and RDQ was confirmed in a combination treatment compared with Limaprost. Physical function of the SF-36 subscales after a combination treatment showed a marked alleviation compared with NSAIDs. Conclusions: These obtained findings suggest that the effects of Limaprost seem to be limited to radicular pain, not for LBP. Overall, a combination treatment might be more effective in the management of radiculopathy induced by LSS than monotherapy with either agent.

A systematic review and meta-analysis of the effectiveness and adverse events of gabapentin and pregabalin for sciatica pain

Aten Primaria 2022 Jan;54(1):102144.PMID:34637958DOI:10.1016/j.aprim.2021.102144.

Aim: This SR aims to assess the effectiveness of pregabalin and gabapentin on pain and disability caused by acute sciatica and the adverse events associated with their clinical use. Design: Systematic review. Databases: Electronic databases of Cochrane Central Register of Controlled Trials, MEDLINE, EMBASE, and Clinical Trials.gov were searched from their inception until March 1st of 2021. Selection criteria: Randomized trials (RCT) with adults>18 years old with acute sciatica for a minimum of 1 week and a maximum of 1 year (at least moderate pain). Data treatment: The outcomes were pain, disability and adverse events. Data was summarized using odds ratio and mean difference. GRADE was used to calculate the level of evidence. Results: Eight RCT involving 747 participants were included. The effect of pregabalin was assessed in 3 RCT and in one three-arm trial (pregabalin vs Limaprost vs a combination of Limaprost and pregabalin). Two trials assessed the effect of gabapentin compared with placebo and one compared with tramadol. One study assessed the effect of gabapentin vs pregabalin in a crossover head-to-head trial. A statistically significant improvement on leg pain at 2 weeks and leg pain with movement at 3 and 4 months was found in a RCT comparing gabapentin with placebo. There were no statistically differences on the remaining time periods assessed for leg pain, low back pain and functional disability. Conclusions: This SR provides clear evidence for lack of effectiveness of pregabalin and gabapentin for sciatica pain management. In view of this, its routine clinical use cannot be supported.

Limaprost reduces motor disturbances by increasing the production of insulin-like growth factor I in rats subjected to spinal cord injury

Transl Res 2010 Nov;156(5):292-301.PMID:20970752DOI:10.1016/j.trsl.2010.08.002.

Calcitonin gene-related peptide (CGRP) released from sensory neurons increases the production of a neuroprotective substance insulin-like growth factor I (IGF-I), and sensory neuron stimulation contributes to a reduction of spinal cord injury (SCI) by inhibiting inflammatory responses in rats. Because receptors for prostaglandin E₂ (EP receptors) are present on sensory neurons, it is possible that prostaglandin E₁ analog Limaprost reduces SCI by increasing IGF-I production through sensory neuron stimulation. We examined this possibility in rats subjected to compression-trauma-induced SCI. Limaprost increased the CGRP release from dorsal root ganglion (DRG) neurons isolated from rats, and this increase was reversed by pretreatment with the EP4 receptor antagonist ONO-AE3-208. Spinal cord tissue levels of CGRP and IGF-I were increased after the induction of SCI, peaking at 2 h postinduction. The intravenous administration of Limaprost enhanced increases of spinal cord tissue levels of CGRP, IGF-I, and IGF-I mRNA at 2 h after the induction of SCI. Increases of spinal cord tissue levels of tumor necrosis factor, caspase-3, myeloperoxidase, and the number of apoptotic nerve cells were inhibited by the administration of Limaprost. Motor disturbances of hind legs in animals subjected to the compression-trauma-induced SCI were reduced by the administration of Limaprost. These effects of Limaprost were reversed completely by pretreatment with a specific transient receptor potential vanilloid 1 inhibitor SB366791 and by sensory denervation. These observations strongly suggest that Limaprost may increase the IGF-I production by stimulating sensory neurons in the spinal cord, thereby ameliorating compression-trauma-induced SCI through attenuation of inflammatory responses.