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马来酸氟吡汀

更新时间:2024-09-10 13:42:11

常用名 马来酸氟吡汀 CAS号 75507-68-5
价格 ¥需询单/1kg ¥需询单/100g ¥需询单/100kg ¥需询单/1ton 纯度 98.0%
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用途:
Flupirtine Maleate(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.IC50 Value: Target: Potassium channel; NMDA receptorin 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 [1]. Therapeutic flupirtine concentrations (≤10 μM) 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 [2]. 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 [4].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 [3]. Both morphine (ED50=0.74 mg/kg) and flupirtine (ED50=3.32 mg/kg) caused dose-related anti-hyperalgesia at doses that did not cause sedation [5]. Toxicity: Based on study-end data, hepatotoxicity was detected in 31% of patients receiving flupirtine for ≥ 6 weeks [6].
物理化学性质:
CAS号:75507-68-5
常用中文名:马来酸氟吡汀
常用英文名:Flupirtine maleate
分子式:C19H21FN4O6
分子量:420.392
密度:1.35 g/cm3
沸点:434.9ºC at 760 mmHg
熔点:186-188ºC
闪点:216.8ºC
储存条件:2-8°C

供应商信息

上海亚兴生物医药科技有限公司

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上海亚兴生物医药科技有限公司于2014年5月成立,是一家专业从事生物医药的研发、生产和销售的企业。 公司目前有两个生产基地,分别在江苏南通市和江苏徐州市。上海拥有3000平方的研发中心,公司目前拥有研发生产团队100余人,博士5人。主要以工业自动化为研究对象,生产高纯度、高产量、高稳定性的产品。公司具备先进检测设备,包括HPLC,GC,TLC,MS 等。目前生产基地都是以先进的流体自动化反应设备为主,包括流动相氢化,酯化,溴化,脱水等自动化生产设备。公司致力于先进自动化设备研发,替代传统反应器。以技术为驱动力,以客户需求为导向,为客户提供更快捷高效的服务,通过不断的生产实践,实现生物医药绿色工艺,为社会创造价值。
上海亚兴生物为客户提供各类氘代化合物的定制服务,产品包括氘代医药中间体,氘代OLED材料等。同时也承接各类医药企业产品生产,工艺开发等。
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参考价格:$66/10mM*1mLinDMSO
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