Title: Bencycloquidium bromide, a novel anti-muscarinic drug, has little effect on central nervous system (CNS) due to its low CNS permeability
Allergic rhinitis(AR)has become a public health problem worldwide. Bencycloquidium bromide(BCQB)，a novel muscarinic receptor antagonist，can be used for the clinical treatment of rhinitis. However，its effect on central nervous system(CNS)has not been clarified. BCQB was intranasally administered at 5.86，2.93 and 1.47mg/kg once a day for 1 month in mice. The effect of this drug on the behavior of mice was investigated by spontaneous activity count，pole test，Morris water maze test and step-down test. The brain tissues and blood plasma of mice were collected at 5min，10min，20min，45min，1.5h，3h，6h，12h and 24h after the administration of BCQB 5.86mg/kg and the concentration of BCQB was analyzed by the method of liquid chromatography-electrospray ionization-mass spectrometry(LC-ESI-MS). There was no significant change in the behavior of mice after the administration of different doses of BCQB(P>0.05). The concentration of BCQB in the brain homogenates at all time points was less than the lower limit of quantification(0.5405ng/ml)，while the concentration of BCQB in blood plasma was 3.86±0.42ng/ml 24h post-administration. These results suggest that BCQB has little effect on CNS in mice，likely due to the fact that BCQB has low CNS permeability.
生物活性 过敏性鼻炎 毒蕈碱 受体拮抗剂 质谱分析
Juan Li Jun-Qing Yang Li Ding Yuan-Da Zhou
1Laboratory of Clinical Pharmacology, the First Affiliated Hospital ofChongqing Medical University, Department of pharmacology of Chongqing Medical University, Chongqing 400016, China Department of Pharmaceutical Analysis, China PharmaceuticalUniversity, 24 Tongjiaxiang, Nanjing 2100
国内会议
石家庄
英文
1-27
2008-10-18（万方平台首次上网日期，不代表论文的发表时间）