生物活性 | |||
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描述 | Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and is used in the treatment of acute circulatory shock. Chlorambucil (CHL), an alkylating agent, as the model therapeutic agent, and used scopine as a novel brain-targeting moiety. The tissue distribution study after i.v. injection revealed that the AUC0-t and Cmax of CHLS in the brain were 14.25- and 12.20-fold of CHL, respectively. Specifically, CHLS (Chlorambucil-Scopine) accumulated in bEnd.3 and C6 cells in an energy-dependent manner. In C6 cells, superior anti-glioma activity with a significantly decreased IC50 of 65.42 nM/mL was observed for CHLS compared to CHL (IC50 > 400 nM/mL). Scopine is a potential brain-targeting moiety for enhancing the brain uptake efficiency of CHL (chlorambucil)[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.44mL 1.29mL 0.64mL |
32.22mL 6.44mL 3.22mL |
64.44mL 12.89mL 6.44mL |
参考文献 |
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