Piribedil hydrochloride 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 hydrochloride 也是一种 α2-肾上腺素受体 (α2-adrenoceptors) 拮抗剂。Piribedil hydrochloride 可抑制 MLL1 甲基转移酶的活性 (EC50: 0.18 μM)。Piribedil hydrochloride 可用于研究帕金森病，循环系统疾病，癌症。
| 生物活性 | Piribedil hydrochloride is a potent and orally activedopamine D2anddopamine D3agonist. Piribedil hydrochloride is also aα2-adrenoceptorsantagonist. Piribedil hydrochloride can inhibitMLL1methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Piribedil hydrochloride (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation[4].
Piribedil hydrochloride (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 hydrochloride (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. |
|
体内研究
(In Vivo) | Piribedil hydrochloride (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in rats model of Parkinson’s disease[2].
Piribedil hydrochloride (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets[3].
Piribedil hydrochloride (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. |
|
| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com