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Flupirtine
NMR and HPLC COA下载 MSDS下载 - Names：
Flupirtine
- CAS号：
56995-20-1
MDL Number： - MF(分子式)： C15H17FN4O2 MW(分子量)： 304.32
- EINECS: Reaxys Number:
- Pubchem ID: Brand:BIOFOUNT
| 货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
|---|---|---|---|---|---|---|---|---|
| YZM010433-10mg | 10mg | ¥ 483.75 | ¥ 483.75 | Backorder | ¥ 0.00 |
| 中文别名 | Flupirtine(cas:56995-20-1) |
| 英文别名 | Flupirtine,56995-20-1 |
| CAS号 | 56995-20-1 |
| Inchi | InChI=1S/C15H17FN4O2/c1-2-22-15(21)19-12-7-8-13(20-14(12)17)18-9-10-3-5-11(16)6-4-10/h3-8H,2,9H2,1H3,(H,19,21)(H3,17,18,20) |
| InchiKey | JUUFBMODXQKSTD-UHFFFAOYSA-N |
| 分子式 Molecular Weight | C15H17FN4O2 |
| 分子量 Formula | 304.32 |
| 溶解度Solubility | No data available |
| 性状 | Solid |
| 储藏条件 Storage conditions | 请根据产品建议的存储条件进行存储，Please store the product under the recommended condition sin the description. |
Flupirtine(CAS:56995-20-1)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
| 产品说明 | (CAS:56995-20-1)Flupirtine(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. IC50 Value: |
| Introduction | 56995-20-1;Flupirtine(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. IC50 Value: Target: Potassium channel; NMDA receptor in vitro: High concentrations of flupirtine antagonized inward currents to NMDA(200 microM) at -70 mV with an lC50 against steady-state responses of 182.1+/-12.1 microM. The effects of flupirtine were voltage-independent and not associated with receptor desensitization making actions within the NMDA receptor channel or at the glycine modulatory site unlikely. NMDA receptor antagonism probably has little relevance for the clinical efficacy of flupirtine as the concentrations needed were far higher than those achieved in clinical practice. However, the activation of a G-protein-regulated inwardly rectifying K+ channel was identified as an interesting molecular target site of flupirtine. In the next stage, the central nervous spectrum of action of experimental K+ channel openers (PCO) was considered. As far as they have been studied, experimental K+ channel openers display a spectrum of action comparable to that of flupirtine . Therapeutic flupirtine concentrations (≤10 M) did not affect voltage-gated Na(+) or Ca(2+) channels, inward rectifier K(+) channels, nicotinic acetylcholine receptors, glycine or ionotropic glutamate receptors. Flupirtine shifted the gating of K(V)7 K(+) channels to more negative potentials and the gating of GABA(A) receptors to lower GABA concentrations . Cell exposure to flupirtine decreased the amplitude of delayed rectifier K(+) current (I(K(DR))) with a concomitant raise in current inactivation in NSC-34 neuronal cells . in vivo: Rats were trained to discriminate the novel analgesic flupirtine (10.0 mg/kg i.p., 10 min) from no drug under a two-choice fixed-ratio 5 shock-termination schedule. Flupirtine yielded a dose-response curve with an ED50 of 3.87 mg/kg. The opioid analgesics pentazocine, codeine and tramadol failed to produce flupirtine appropriate responding. The opioid antagonist naltrexone did not antagonize the discriminative effects of flupirtine . Both morphine (ED =0.74mg/kg) and flupirtine (ED=3.32mg/kg) caused dose-related anti-hyperalgesia at doses that did not cause sedation . Toxicity: Based on study-end data, hepatotoxicity was detected in 31% of patients receiving flupirtine for ≥ 6 weeks . |
| Application1 | |
| Application2 | |
| Application3 |
| 警示图 | |
| 危险性 | warning |
| 危险性警示 | Not available |
| 安全声明 | H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害 |
| 安全防护 | P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理 |
| 备注 | 实验过程中防止吸入、食入，做好安全防护 |
| 【1】.Kornhuber J, et al. Flupirtine shows functional NMDA receptor antagonism by enhancing Mg2+ block via activation of voltageindependent potassium channels. Rapid communication. J Neural Transm. 1999;106(9-10):857-67. |
| 【2】.Klinger F, et al. Concomitant facilitation of GABAA receptors and KV7 channels by the non-opioid analgesic flupirtine. Br J Pharmacol. 2012 Jul;166(5):1631-42. |
| 【3】.Swedberg MD, et al. Pharmacological mechanisms of action of flupirtine: a novel, centrally acting, nonopioid analgesic evaluated by its discriminative effects in the rat. J Pharmacol Exp Ther. 1988 Sep;246(3):1067-74. |
| 【4】.Wu SN, et al. Evidence for inhibitory effects of flupirtine, a centrally acting analgesic, on delayed rectifier k(+) currents in motor neuron-like cells. Evid Based Complement Alternat Med. 2012;2012:148403. |
| 【5】.Kolosov A, et al. Flupirtine enhances the anti-hyperalgesic effects of morphine in a rat model of prostate bone metastasis. Pain Med. 2012 Nov;13(11):1444-56. |
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