产品
编 号:F568954
分子式:C16H18N4O2
分子量:298.34
产品类型
结构图
CAS No: 3605-01-4
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产品详情
生物活性:
Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
体内研究:
Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease.Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets.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.Animal Model:Rat model of Parkinson’s disease
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
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.
体外研究:
Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation.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.Piribedil (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11).