生物活性 | |||
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描述 | Phenylethanolamine-N-methyltransferase (PNMT) is an enzyme that catalyzes the final step of the biosynthesis of epinephrine from norepinephrine. LY 78335 is a PNMT inhibitor with a Ki value of 0.09μM in vitro. The half-life of LY 78335 in rat adrenal glands after injection of a dose of 0.2mmol/kg was 3.4 hours. Treatment of rats with 0.2mmol/kg LY 78335 1 hour before forced exercise led to a significant reduction in the epinephrine level compared with the saline-treated controls[1]. Treatment of mice with 25mg/kg LY 78335 resulted in dose-related reductions in exploratory head-dipping in the hold-board test without affecting locomotor activity[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.41mL 0.88mL 0.44mL |
22.07mL 4.41mL 2.21mL |
44.14mL 8.83mL 4.41mL |
参考文献 |
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