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目的研究5-HT1A受体激动和5-HT重摄取抑制双靶标新药YL-0919在小鼠体内的组织分布特征。方法 15只雄性昆明小鼠随机分为3组,单剂量YL-0919(6 mg/kg)灌胃后,分别于2,5,60 min摘眼球取血,处死后解剖取组织。采用液相色谱串联质谱法测定YL-0919浓度。结果小鼠YL-0919灌胃后2 min即在小肠、胃和肝达到最高值,其他组织在给药后5 min浓度达到最高值,浓度由高到低依次为:小肠>胃>肝脏>脂肪>肾脏>肺脏>心脏>脾脏>血>脑>肌肉>睾丸,60 min后各组织的药物浓度均降至较低水平。结论 YL-0919在小鼠体内的吸收和分布较快,药物入血后很快分布到体内各个组织中;药物在组织中的消除也较快,没有组织蓄积现象。
Objective To investigate the tissue distribution characteristics of 5-HT1A receptor agonist and 5-HT reuptake inhibitor YL-0919 in mice. Methods Fifteen male Kunming mice were randomly divided into three groups. After a single dose of YL-0919 (6 mg / kg) was given into the stomach, blood was taken from the eyeballs at 2,5,60 min, and the tissues were dissected after sacrifice. The concentration of YL-0919 was determined by liquid chromatography tandem mass spectrometry. Results The maximal value of the intestine, stomach and liver reached the maximum at 2 min after intragastric administration of YL-0919. The highest concentration of other tissues reached the maximum at 5 min after administration, with the order from high to low: small intestine> stomach> liver> fat > Kidney> lung> heart> spleen> blood> brain> muscle> testis. After 60 min, the drug concentration in each tissue was reduced to a lower level. Conclusion The absorption and distribution of YL-0919 in mice are fast. The drugs are rapidly distributed to various tissues in the body after they enter the bloodstream. The elimination of drugs in the tissues is also faster and there is no accumulation of tissue.