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Title: Bencycloquidium bromide, a novel anti-muscarinic drug, has little effect on central nervous system (CNS) due to its S permeability
Authors: Juan Li 1, Jun-Qing Yang2 , Li Ding3, Yuan-Da Zhou1﹡
Running title: S permeability of bencycloquidium bromide
Address: 1Laboratory of Clinical Pharmacology, the First Affiliated Hospital of Chongqing Medical University, Chongqing 400016, China
2Department of pharmacology of Chongqing Medical University, Chongqing 400016, China
3Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China
﹡ Correspondence to: Department of Clinical Pharmacology, the First Affiliated Hospital of Chongqing Medical University, Chongqing 400016, China. Tel: 86-23-68898185; fax: 86-23-68898185.
Email address: zpsecond@
ABSTRACT
Allergic rhinitis (AR) has e 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 , and 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, , 3h, 6h, 12h and 24h after the administration of BCQB 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 > ). The concentration of BCQB in the brain homogenates at all time points was less than the lower limit of quantification (), while the concentration of BCQB in blood plasma was ± 24h post-administration. These results sugges