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Antrafenine Sale

(Synonyms: 安曲非宁; Stakane) 目录号 : GC63618

Antrafenine (Stakane) 是一种非麻醉性缓解疼痛试剂,在药理学和毒理学研究中表现出长时间的作用和良好的耐受性。

Antrafenine Chemical Structure

Cas No.:55300-29-3

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5 mg
¥13,500.00
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产品描述

Antrafenine (Stakane) is a non-narcotic analgesic, shows long duration of action, and excellent tolerance in pharmacological and toxicological studies[1][2].

[1]. Manoury PM, et al. Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates. J Med Chem. 1979;22(5):554-559.

Chemical Properties

Cas No. 55300-29-3 SDF
别名 安曲非宁; Stakane
分子式 C30H26F6N4O2 分子量 588.54
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1 mM 1.6991 mL 8.4956 mL 16.9912 mL
5 mM 0.3398 mL 1.6991 mL 3.3982 mL
10 mM 0.1699 mL 0.8496 mL 1.6991 mL
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Research Update

Antrafenine, naproxen and placebo in osteoarthritis: a comparative study

Br J Rheumatol 1983 May;22(2):89-94.PMID:6342700DOI:10.1093/rheumatology/22.2.89.

Antrafenine is a new non-narcotic analgesic. In a double-blind, cross-over study the efficacy of Antrafenine at doses of 450 mg/day and 900 mg/day was compared to naproxen 750 mg/day and placebo in patients with osteoarthritis. Each drug treatment was given for two weeks, the total duration of the study being eight consecutive weeks. Antrafenine, at either dose, was effective in relieving pain associated with osteoarthritis; the efficacy was comparable to naproxen. There was no definite indication that 900 mg/day was more effective than 450 mg/day. Antrafenine, at both dosage levels, was well tolerated. Any noted side-effects were mild. There was a total of 12 side-effects in nine patients with the high dose, five side-effects in five patients with the low dose, compared with 11 side-effects in nine patients with naproxen and 10 side-effects in seven patients with placebo.

Antrafenine: anti-inflammatory activity with respect to oedema and leucocyte infiltration in the rat

Agents Actions 1984 Feb;14(2):296-9.PMID:6608864DOI:10.1007/BF01966656.

Antrafenine effectively suppressed carrageenan paw oedema in the rat (ED 40 = 24 mg/kg p.o) in the dose range of 10-40 mg/kg p.o, approximating that of phenylbutazone. Antrafenine was superior to phenylbutazone with respect to inhibition of exudate volume and total leucocyte infiltration in carrageenan and calcium pyrophosphate dihydrate crystal pleurisies. The effect of Antrafenine on leucocytes was most striking, significant suppression being observed at each dose tested (10, 20, 40 mg/kg p.o), whereas phenylbutazone showed significant activity only at the relatively elevated dose of 40 mg/kg p.o. These observations suggest that Antrafenine merits further investigation with respect to its anti-inflammatory effects.

Home Treatment of Older People with Symptomatic SARS-CoV-2 Infection (COVID-19): A structured Summary of a Study Protocol for a Multi-Arm Multi-Stage (MAMS) Randomized Trial to Evaluate the Efficacy and Tolerability of Several Experimental Treatments to Reduce the Risk of Hospitalisation or Death in outpatients aged 65 years or older (COVERAGE trial)

Trials 2020 Oct 13;21(1):846.PMID:33050924DOI:10.1186/s13063-020-04619-1.

Objectives: To assess the efficacy of several repurposed drugs to prevent hospitalisation or death in patients aged 65 or more with recent symptomatic SARS-CoV-2 infection (COVID-19) and no criteria for hospitalisation. Trial design: Phase III, multi-arm (5) and multi-stage (MAMS), randomized, open-label controlled superiority trial. Participants will be randomly allocated 1:1:1:1:1 to the following strategies: Arm 1: Control arm Arms 2 to 5: Experimental treatment arms Planned interim analyses will be conducted at regular intervals. Their results will be reviewed by an Independent Data and Safety Monitoring Board. Experimental arms may be terminated for futility, efficacy or toxicity before the end of the trial. New experimental arms may be added if new evidence suggests that other treatments should be tested. A feasibility and acceptability substudy as well as an immunological substudy will be conducted alongside the trial. Participants: Inclusion criteria are: 65-year-old or more; Positive test for SARS-CoV-2 on a nasopharyngeal swab; Symptoms onset within 3 days before diagnosis; No hospitalisation criteria; Signed informed consent; Health insurance. Exclusion criteria are: Inability to make an informed decision to participate (e.g.: dementia, guardianship); Rockwood Clinical Frailty Scale ≥7; Long QT syndrome; QTc interval > 500 ms; Heart rate <50/min; Kalaemia >5.5 mmol/L or <3.5 mmol/L; Ongoing treatment with piperaquine, halofantrine, dasatinib, nilotinib, hydroxyzine, domperidone, citalopram, escitalopram, potent inhibitors or inducers of cytochrome P450 CYP3A4 isoenzyme, repaglinide, azathioprine, 6-mercaptopurine, theophylline, pyrazinamide, warfarin; Known hypersensitivity to any of the trial drugs or to chloroquine and other 4-aminoquinolines, amodiaquine, mefloquine, glafenine, floctafenine, Antrafenine, ARB; Hepatic porphyria; Liver failure (Child-Pugh stage ≥B); Stage 4 or 5 chronic kidney disease (GFR <30 mL/min/1.73 m²); Dialysis; Hypersentivity to lactose; Lactase deficiency; Abnormalities in galactose metabolism; Malabsorption syndrome; Glucose-6-phosphate dehydrogenase deficiency; Symptomatic hyperuricemia; Ileus; Colitis; Enterocolitis; Chronic hepatitis B virus disease. The trial is being conducted in France in the Bordeaux, Corse, Dijon, Nancy, Paris and Toulouse areas as well as in the Grand Duchy of Luxembourg. Participants are recruited either at home, nursing homes, general practices, primary care centres or hospital outpatient consultations. Intervention and comparator: The four experimental treatments planned in protocol version 1.2 (April 8th, 2020) are: (1) Hydroxychloroquine 200 mg, 2 tablets BID on day 0, 2 tablets QD from day 1 to 9; (2) Imatinib 400 mg, 1 tablet QD from day 0 to 9; (3) Favipiravir 200 mg, 12 tablets BID on day 0, 6 tablets BID from day 1 to 9; (4) Telmisartan 20 mg, 1 tablet QD from day 0 to 9. The comparator is a complex of vitamins and trace elements (AZINC Forme et Vitalité®), 1 capsule BID for 10 days, for which there is no reason to believe that they are active on the virus. In protocol version 1.2 (April 8th, 2020): People in the control arm will receive a combination of vitamins and trace elements; people in the experimental arms will receive hydroxychloroquine, or favipiravir, or imatinib, or telmisartan. Main outcome: The primary outcome is the proportion of participants with an incidence of hospitalisation and/or death between inclusion and day 14 in each arm. Randomisation: Participants are randomized in a 1:1:1:1:1 ratio to each arm using a web-based randomisation tool. Participants not treated with an ARB or ACEI prior to enrolment are randomized to receive the comparator or one of the four experimental drugs. Participants already treated with an ARB or ACEI are randomized to receive the comparator or one of the experimental drugs except telmisartan (i.e.: hydroxychloroquine, imatinib, or favipiravir). Randomisation is stratified on ACEI or ARBs treatment at inclusion and on the type of residence (personal home vs. nursing home). Blinding (masking): This is an open-label trial. Participants, caregivers, investigators and statisticians are not blinded to group assignment. Numbers to be randomised (sample size): A total of 1057 participants will be enrolled if all arms are maintained until the final analysis and no additional arm is added. Three successive futility interim analyses are planned, when the number of participants reaches 30, 60 and 102 in the control arm. Two efficacy analyses (interim n°3 and final) will be performed successively. Trial status: This describes the Version 1.2 (April 8th, 2020) of the COVERAGE protocol that was approved by the French regulatory authority and ethics committee. The trial was opened for enrolment on April 15th, 2020 in the Nouvelle Aquitaine region (South-West France). Given the current decline of the COVID-19 pandemic in France and its unforeseeable dynamic in the coming months, new trial sites in 5 other French regions and in Luxembourg are currently being opened. A revised version of the protocol was submitted to the regulatory authority and ethics committee on June 15th, 2020. It contains the following amendments: (i) Inclusion criteria: age ≥65 replaced by age ≥60; time since first symptoms <3 days replaced by time since first symptoms <5 days; (ii) Withdrawal of the hydroxychloroquine arm (due to external data); (iii) increase in the number of trial sites. Trial registration: The trial was registered on Clinical Trials.gov on April 22nd, 2020 (Identifier: NCT04356495): and on EudraCT on April 10th, 2020 (Identifier: 2020-001435-27). Full protocol: The full protocol is attached as an additional file, accessible from the Trials website (Additional file 1). In the interest of expediting dissemination of this material, the familiar formatting has been eliminated; this Letter serves as a summary of the key elements of the full protocol. The study protocol has been reported in accordance with the Standard Protocol Items: Recommendations for Clinical Interventional Trials (SPIRIT) guidelines (Additional file 2).

Assessment of analgesic drugs in soft tissue injuries presenting to an accident and emergency department--a comparison of Antrafenine, paracetamol and placebo

Postgrad Med J 1982 Aug;58(682):489-92.PMID:6752926DOI:10.1136/pgmj.58.682.489.

In a preliminary dose-finding study in patients following abdominal hysterectomy, Antrafenine was found to be an effective analgesic in single oral doses of 300-600 mg. A double-blind controlled between-patient study was carried out to compare Antrafenine (up to 1200 mg daily), paracetamol (up to 4 g daily) and placebo as analgesic in the control of pain produced by ligamentous knee or ankle injuries, low back pain or rib injuries. The only significant difference (P<0·05) noted between drug treatments was a longer duration of analgesic activity following Antrafenine. The implications of these results for the study of potential analgesic drugs in soft tissue injuries are discussed.

In silico identification of new inhibitors for βeta-2-glycoprotein I as a major antigen in antiphospholipid antibody syndrome

J Mol Model 2020 May 26;26(6):156.PMID:32458176DOI:10.1007/s00894-020-04406-4.

Beta 2 glycoprotein I (β2GPI) is a major antigen for autoantibodies present in antiphospholipid antibody syndrome (APS). β2GPI is a single polypeptide with five repeated domains and different conformations. The activated J-shaped conformation of β2GPI binds to negatively charged phospholipids in the membrane via the fifth domain and causes blood clotting reactions. We applied a drug repurposing strategy using virtual screening and molecular dynamics to find the best FDA drugs against the fifth domain of β2GPI. In the first phase, FDA drugs that had the most favorable ΔG with the fifth domain of β2GPI were selected by virtual screening. Among these drugs that had the most favorable ΔG, Vorapaxar and Antrafenine were selected for molecular dynamics (MD) simulation studies. MD simulation was performed to evaluate the stability of Vorapaxar and Antrafenine complexes and the effect of the two drugs on protein conformation. Also, MD simulation was done to investigate the effect of Antrafenine and Vorapaxar on the binding of β2GPI to the platelet model membrane. According to the results, Vorapaxar and Antrafenine were bound to the protein with the favorable binding energy (Vorapaxar and Antrafenine binding energies are - 49.641 and - 38.803 kcal/mol, respectively). In this study, it was shown that unlike protein alone and protein in the Antrafenine complex, the protein in the Vorapaxar complex was completely separated from the model membrane after 350 ns. Moreover, Vorapaxar led to more changes in the activated J-shape of β2GPI. Thus, Vorapaxar can be a suitable candidate for further investigations on the treatment of APS.