Piribedil 是一种有效且具有口服活性的多巴胺 D2 (dopamine D2) 和 多巴胺 D3 (dopamine D3) 激动剂。Piribedil 也是一种 α2-肾上腺素受体 (α2-adrenoceptors) 拮抗剂。Piribedil 可抑制 MLL1 甲基转移酶的活性 (EC50: 0.18 μM)。Piribedil 可用于研究帕金森病，循环系统疾病，癌症。
| 生物活性 | Piribedil is a potent and orally activedopamine D2anddopamine D3agonist. Piribedil is also aα2-adrenoceptorsantagonist. Piribedil can inhibitMLL1methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4]. |
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体外研究
(In Vitro) | Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation[4].
Piribedil (0-160 μM, 4 days) selectively decreases the H3K4 methylation in MLL-r cells (THP-1 and MV4;11), by disturbing the MLL1-WDR5 interaction[4].
Piribedil (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11)[4].
Cell Proliferation Assay[4] | Cell Line: | MLL-r AML cells (THP-1 and MV4;11), non-MLL leukemia cell line (K562) | | Concentration: | 0, 20, 40, 80 and 160 μM | | Incubation Time: | 0-7 days | | Result: | Inhibited the growth rate of the THP-1 and MV4;11 cells in a time-dependent manner. |
Western Blot Analysis[4] | Cell Line: | THP-1 and MV4;11 cells | | Concentration: | 0, 20, 40, 80 and 160 μM | | Incubation Time: | 4 days | | Result: | Decreased the levels of H3K4me2 and H3K4me3 without affecting the methylation of other histones, such as H3K79, H3K36 and H3K27. |
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体内研究
(In Vivo) | Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease[2].
Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets[3].
Piribedil (oral gavage, 150 mg/kg, daily for 21 days) inhibits MLL-r tumor growth and decreases the expression of MLL1 target genes in MV4;11 tumor xenografts[4].
| Animal Model: | Rat model of Parkinson’s disease[2] | | Dosage: | 5, 15, 40 mg/kg | | Administration: | intraperitoneal injection, administered 5 min before administration of L-DOPA. | | Result: | Reduced turning behaviour and AD (axial dystonia), OD (orolingual dyskinesia) and FD (forelimb dyskinesia) at 5 and 40 mg/kg.
Increased LD (locomotive dyskinesias) at the 40 mg/kg. |
| Animal Model: | Adult common marmosets[3] | | Dosage: | 4-5 mg/kg | | Administration: | Oral gavage, daily for 2 weeks | | Result: | Increased vigilance and alertness and reversed the downregulation of preprotachykinin mRNA induced by MPTP in rostral and caudal striatum. |
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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 : 33.33 mg/mL(111.72 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.3519 mL | 16.7594 mL | 33.5188 mL | | 5 mM | 0.6704 mL | 3.3519 mL | 6.7038 mL | | 10 mM | 0.3352 mL | 1.6759 mL | 3.3519 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.38 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.38 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.38 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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