Biperiden (KL 373) 是一种非选择性毒蕈碱受体 (muscarinic receptor) 拮抗剂，可以与M1毒蕈碱受体竞争性结合，从而抑制乙酰胆碱 (acetylcholine) 并增强中枢神经系统中多巴胺信号传导。 Biperiden 可用于帕金森病以及其他相关精神疾病的研究。
| 生物活性 | Biperiden (KL 373) is a non-selectivemuscarinic receptorantagonist that competitively binds toM1muscarinic receptors, thereby inhibitingacetylcholineand enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders[1][2]. |
体外研究
(In Vitro) | Biperiden (29.6 μg/ml, 72 hours) can significantly induce apoptosis and inhibit proliferation at high doses in human pancreatic ductal adenocarcinoma cells[1].
Cell Proliferation Assay[1] | Cell Line: | Panc-1, Panc-2 and BxPC3 human pancreatic ductal adenocarcinoma cells | | Concentration: | 29.6 μg/mL | | Incubation Time: | 72 hours | | Result: | Inhibited cell proliferation at 72 hours significantly by reducing nuclear c-Rel translocation. |
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体内研究
(In Vivo) | Biperiden (intraperitoneal injection, 10 mg/kg, everyday, 3 weeks) reduces tumor size by 83% in subcutaneous xenograft mouse using Panc-1 human pancreatic ductal adenocarcinoma cells[1].
Biperiden (intraperitoneal injection, 8 mg/kg, every 8 hours, 10 days) can reduce frequency of spontaneous seizures and extracellular hippocampal glutamate levels while cause a long-term decrease in hippocampal excitability[2].
| Animal Model: | Subcutaneous xenograft mouse using Panc-1 human pancreatic ductal adenocarcinoma cells[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; everyday; 3 weeks | | Result: | Tumor size reduced by 83%. |
| Animal Model: | Male Wistar rats (200-250 g)[2] | | Dosage: | 8 mg/kg | | Administration: | Intraperitoneal injection; every 8 hours; 10 days | | Result: | Reduced late seizures by about three times with no affecting emotional memory damage. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(160.53 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2107 mL | 16.0534 mL | 32.1069 mL | | 5 mM | 0.6421 mL | 3.2107 mL | 6.4214 mL | | 10 mM | 0.3211 mL | 1.6053 mL | 3.2107 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
