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152±23μM)阻断。酮色林(50-350μM)通过以剂量依赖性方式阻断受体来抑制协同作用。 Cyproheptadine的IC50值为22±7μM,Ketanserin的IC50值为152±23μM[2]。酮色林抑制血小板聚集,IC50为240(169-339)nM [3]。",{"key":249,"value":250},"体内研究","酮色林是5-HT2A受体拮抗剂。 Ketanserin显着降低许多大脑区域(海马CA1和CA3,前额叶皮质,中央杏仁核,背内侧下丘脑核,齿状回,伏隔核和中脑导水管周围灰质)的BDNF蛋白水平。 5-HT2A拮抗剂Ketanserin可以显着降低各脑区的BDNF mRNA水平[4]。",{"key":252,"value":253},"细胞实验","将建立的稳定表达hERG通道的HEK 293细胞系在补充有10％胎牛血清，400μg\u002F mL G418的Dulbecco改良的Eagle培养基（DMEM）中培养。稳定表达重组人心脏KCNQ1 \u002F KCNE1通道电流（IKs）的HEK 293细胞系维持在含有10％胎牛血清和100μg\u002F mL潮霉素的DMEM中。将用于电生理学的细胞接种在玻璃盖玻片上。构建突变体hERG通道，并使用10μLLipofectamine2000和pCDNA3载体中的4μghERG突变体cDNA在HEK 293细胞中瞬时表达[1]。",{"key":255,"value":256},"动物实验","大鼠[4]使用总共155只无特定病原体的2月龄雄性Sprague-Dawley大鼠，体重180-220g。将大鼠随机分为以下六组：5-HT1A受体激动剂（8-OH-DPAT）PS组（DPAT-PS组，n = 30）; 5-HT1A受体拮抗剂（MDL73005）PS组（MDL-PS组，n = 30）; 5-HT2A受体激动剂（DOI）PS组（DOI-PS组，n = 30）; 5-HT2A受体拮抗剂（Ketanserin）PS组（Ketan-PS组，n = 30）;溶剂对照无应激组（0.9％生理盐水组，CON组）;和仅PS组（PS组，n = 30）。根据应力和分析之间的时间，将DPAT-PS，MDL-PS，DOI-PS，Ketan-PS和PS组进一步分为六个亚组（每组n = 5）;压力后立即，压力后0.5,1,2,6和24小时。 CON组（n = 5）接收正常饲料。对于Ketan-PS组，溶解于0.9％生理盐水中的酮色林在每次应激暴露前1小时以5mg \u002F kg腹膜内注射。",{"key":258,"value":259},"参考文献","[1].\nTang Q, et al. The 5-HT2 antagonist Ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels. Br J Pharmacol. 2008 Oct;155(3):365-73.\n[2].\nKhan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergistic interaction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506.\n[3].\nKekewska A, et al. Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol Exp Ther. 2012 Feb;340(2):369-76.\n[4].\nJiang DG, et al. Serotonin regulates brain-derived neurotrophic factor expression in select brain regions during acute psychological stress. 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