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    • 2. 发明授权
    • Application of puerarin in the preparation of P2X3 mediated drugs for pain/nervous system diseases
    • 应用葛根素制备P2X3介导的药物用于疼痛/神经系统疾病
    • US08362070B2
    • 2013-01-29
    • US12922245
    • 2010-06-29
    • Shangdong LiangChangshui XuYun GaoGuilin LiJiari LinShuangmei LiuHan LiuJun ZhangXin Li
    • Shangdong LiangChangshui XuYun GaoGuilin LiJiari LinShuangmei LiuHan LiuJun ZhangXin Li
    • A61K31/35A61K31/70
    • A61K31/352
    • The invention relates to the new usage of puerarin in the field of pharmaceutical products, in other words, it relates to the application of puerarin in the preparation of drugs for P2X3 mediated pain/nervous system diseases. The experiment shows that puerarin can inhibit pain-related behavioral responses, subsequently immunohistochemical analysis, in situ hybridization, RT-PCR, protein blotting and other techniques were utilized to observe the inhibition of puerarin on mRNA and protein expression of P2X3 receptor in dorsal root ganglion of rats with neuropathic pain and in dorsal root ganglion and sensory nerve ending in the burn model of rats, it was found by using whole-cell patch clamp technique that puerarin can significantly reduce the electric current activated by P2X3 receptor agonist in the neuron of dorsal root ganglion of rats with neuropathic pain. The experiment proves that the mechanism for the inhibitory effects of puerarin on acute and chronic pain is to block the transmission of pain sense information that is mediated by P2X3 receptor in primary sensory neurons. The invention provides a kind of new method for the prevention and treatment on acute and chronic pain, and it also indicates that puerarin can act as a antagonist for P2X3 receptor, which will be helpful for the application of drugs in the prevention and treatment on P2X3 receptor involved nervous system diseases.
    • 本发明涉及葛根素在药物领域的新用途,换句话说,涉及葛根素在制备P2X3介导的疼痛/神经系统疾病药物中的应用。 实验表明,葛根素可以抑制疼痛相关的行为反应,随后免疫组化分析,原位杂交,RT-PCR,蛋白质印迹等技术用于观察葛根素对背根神经节P2X3受体mRNA和蛋白表达的抑制作用 的大鼠神经性疼痛和背根神经节和感觉神经结束于大鼠烧伤模型,通过使用全细胞膜片钳技术发现,葛根素可以显着降低P2X3受体激动剂在背侧神经元中活化的电流 神经性疼痛大鼠根神经节。 实验证明,葛根素对急性和慢性疼痛的抑制作用机制是阻断P2X3受体介导的疼痛感知信息在原发感觉神经元中的传播。 本发明提供了一种预防和治疗急性和慢性疼痛的新方法,也表明葛根素可以作为P2X3受体的拮抗剂,有利于药物在P2X3的预防和治疗中的应用 受体涉及神经系统疾病。