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Property","水溶解性","水溶性：不溶；易溶于：氯仿；可溶于：醇,苯,乙醚,丙酮",null,[],[243,246,249,252,255,258,261],{"key":244,"value":245},"描述","Imperatorin 是一种有效的 NO synthesis 抑制剂,IC50 为 9.2 μmol,也是 BChE 抑制剂,IC50 为 31.4 μmol。Imperatorin 是 TRPV1 的微弱激动剂,EC50 为 12.6±3.2 μM。",{"key":247,"value":248},"相关类别","信号通路\n>>\n神经信号通路\n>>\n疼痛\n信号通路\n>>\n跨膜转运\n>>\nTRP频道\n天然产物\n>>\n苯丙酸类\n研究领域\n>>\n神经疾病",{"key":250,"value":251},"靶点","IC50: 9.2 μmol (NO synthesis), 31.4 μmol (BChE)[1]EC50: 12.6±3.2 μM (TRPV1)[2]",{"key":253,"value":254},"体外研究","欧前胡素是属于香豆素类-特别是呋喃香豆素类的植物次生代谢产物。欧前胡素通过α1β2γ2S受体增强GABA诱导的氯离子电流(IGABA)。欧前胡素可使IGABA在100μmol下增加50.5±16.3％,在300μmol下增加109.8±37.7％。在白藜芦醇根中发现的欧前胡素和Phellopterin在体外抑制[3H]地西泮与大鼠脑GABAA受体的苯二氮卓位点的结合,欧前胡素的IC50为12.3μmol,Phellopterin的IC50为400nmol。欧前胡素浓度范围为3.5至14毫摩尔,通过与GABA-T的活性位点不可逆地结合,以时间依赖性和浓度依赖性方式显着且不可逆地抑制GABA-T。角质素是一种可逆的乙酰胆碱酯酶(AChE)抑制剂,并以剂量依赖的方式起作用。通过分光光度法在12.5,25,50和100μg\u002F mL的浓度下测试欧前胡素和来自当归果实的粗提取物的AChE和BChE抑制活性。欧前胡素对AChE的抑制率低(13.75-46.11％),而对BChE的抑制作用显着(37.46-83.98％)。欧前胡素对BChE而不是AChE具有选择性,BChE的IC50为31.4μmol。欧前胡素与(+)- Byakangelicol一起被发现是最有效的BACE-1抑制剂,IC50分别为91.8和104.9μmol。欧前胡素(IC50 =9.2μmol)作为NO合成的抑制剂也是有效的[1]。欧前胡素是TRPV1的弱激动剂,TRPV1是一种涉及检测几种有害刺激的通道,其EC50为12.6±3.2μM[2]。",{"key":256,"value":257},"体内研究","在剂量为10和20 mg\u002Fkg且注射后30分钟时,欧前胡素具有抗焦虑作用,并改善记忆和学习过程的不同阶段-包括获得和巩固。还显示以10和20mg\u002Fkg的剂量急性施用欧前胡素降低了尼古丁的致焦虑作用(0.1mg\u002Fkg,皮下,sc)。在30和40 mg\u002Fkg时,腹腔注射欧前胡素可显着增强卡马西平对抗最大电休克诱发癫痫发作的抗惊厥活性,通过将ED50从10.8降低到6.8 mg\u002Fkg(降低34％)和6 mg\u002Fkg(降低42％)来表达。 , 分别。此外,30 mg\u002Fkg的欧前胡素和6.8 mg\u002Fkg的卡马西平显示卡马西平的总脑浓度从1.260增加到2.328μg\u002F mL(增加85％),这可能是由于改变血液屏障渗透性或类似多药耐药蛋白的抑制剂[1]。欧前胡素(一种天然存在的呋喃香豆素)使γ-氨基丁酸转氨酶失活并抑制乙酰胆碱酯酶活性。在注射东莨菪碱(1mg\u002Fkg)之前以5和10mg\u002Fkg的剂量急性施用欧前胡素改善了由东莨菪碱损害的记忆获得和巩固。此外,可重复(7天,每天两次)给予最高剂量的欧前胡素(10mg\u002Fkg)显着减弱东莨菪碱对记忆获得的影响,而5和10mg\u002Fkg这种呋喃香豆素的剂量在记忆时是有效的。合并是衡量的[3]。",{"key":259,"value":260},"动物实验","小鼠[3]实验在重20-25g的幼稚雄性瑞士小鼠上进行。以10mL \u002F kg的体积腹膜内（ip）施用药物。在实验的每一天制备新鲜药物溶液。对照组接受相同体积的盐水注射并通过相同的给药途径。在急性治疗期间，将动物分配到以下药物组：盐水，卡巴拉汀（0.5 mg \u002F kg，ip），东莨菪碱（1 mg \u002F kg，ip），欧前胡素（1,5,10 mg \u002F kg，ip）或欧前胡素与东莨菪碱共同给药。为了测量记忆获取过程，在预测试前20分钟施用东莨菪碱，而在前测试前30分钟施用欧前列素和利凡斯的明。为了测量记忆巩固过程，在预试验后立即给予利凡斯的明或东莨菪碱（1mg \u002F kg），而在预试验后15分钟或东莨菪碱注射后给予欧前胡素。在第二天，小鼠被重新测试。在第二组实验中，动物随机分配接受6天ip注射欧前胡素（1,5和10 mg \u002F kg，ip）或生理盐水，每日两次（上午8:00和晚上8:00） 。在第7天，对这些动物进行盐水，东莨菪碱（1mg \u002F kg，ip），欧前胡素（1,5和10mg \u002F kg，ip），或与东莨菪碱共同施用的欧前胡素。为了测量记忆获取过程，在预测试前20分钟施用东莨菪碱，在预测试前30分钟施用欧前胡素。为了测量记忆巩固过程，在预试验后立即给予东莨菪碱（1mg \u002F kg），而在前测试后15分钟或东莨菪碱注射后给予欧前胡素。在第八天，小鼠被重新测试。",{"key":262,"value":263},"参考文献","[1].\nKozioł E, et al. Imperatorin-pharmacological meaning and analytical clues: profound investigation. Phytochem Rev. 2016;15:627-649.\n[2].\nChen X, et al. Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1 (TRPV1) channel. J Biol Chem. 2014 Apr 4;289(14):9600-10.\n[3].\nBudzynska B, et al. Effects of imperatorin on scopolamine-induced cognitive impairment and oxidative stress in mice. 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