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Piribedil

SKU: orb1225204

Description

Piribedil is an antiparkinsonian agent andpiperazine derivative which acts as a D2 and D3 receptor agonist. It also has α2-adrenergic antagonist properties(In Vitro):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).(In Vivo):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.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Piribedil

Key Properties

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CAS Number3605-01-4
MW298.34
Purity>98% (HPLC)
FormulaC16H18N4O2
SMILESC1(N2CCN(CC3=CC4=C(C=C3)OCO4)CC2)=NC=CC=N1
TargetAdrenergic Receptor
SolubilitySoluble in chloroform, DMSO, Ethanol, Water

Bioactivity

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In Vivo
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.
In Vitro
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). Cell Proliferation Assay 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. 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.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Piribedil | ET 495 | ET-495 | ET495 | EU 4200

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Quality Guarantee

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Quick Database Links

Gene Symbol
Adrenergic Receptor

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