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氟吡汀

氟吡汀用途

Flupirtine(D 9998)是神经元钾通道开放剂,同时还能拮抗NMDA受体。

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氟吡汀名称

[ CAS 号 ]:
56995-20-1

[ 中文名 ]:
氟吡汀

[ 英文名 ]:
Flupirtine

[中文别名 ]:

氟吡啶

[英文别名 ]:

EINECS 260-503-8
Flupirtine
Effirma

氟吡汀生物活性

[ 描述 ]:

Flupirtine(D 9998)是神经元钾通道开放剂,同时还能拮抗NMDA受体。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> iGluR

信号通路 >> 神经信号通路 >> iGluR

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 神经疾病

天然产物 >> 生物碱

[参考文献]

[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.

[6]. Michel MC, et al. Unexpected frequent hepatotoxicity of a prescription drug, flupirtine, marketed for about 30 years. Br J Clin Pharmacol. 2012 May;73(5):821-5.

[相关活性小分子]

氟吡汀物理化学性质

[ 密度 ]:
1.35g/cm3

[ 沸点 ]:
434.9ºC at 760mmHg

[ 熔点 ]:
115 - 116ºC

[ 分子式 ]:
C₁₅H₁₇FN₄O₂

[ 分子量 ]:
304.31900

[ 闪点 ]:
216.8ºC

[ 精确质量 ]:
304.13400

[ PSA ]:
89.27000

[ LogP ]:
3.71060

[ 折射率 ]:
1.661

[ 储存条件 ]:
2-8℃

氟吡汀安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

氟吡汀合成路线

详细合成路线

氟吡汀上下游产品

氟吡汀上游产品

氟吡汀下游产品

氟吡汀制备

2-氨基-3-硝基-6-氯吡啶和对氟苄胺反应，生成的产物再还原、氯甲酸乙酯酰化，最后和马来酸在异丙醇中作用，得马来酸氟吡汀。