1. Piribedil dihydrochloride

Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.

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Piribedil dihydrochloride Chemical Structure

Piribedil dihydrochloride Chemical Structure

CAS No. : 1451048-94-4

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Description

Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].

IC50 & Target

D2R, hα1A-AR[1]
EC50: 0.18 μM (MLL1 methyltransferase)[4]

In Vitro

Piribedil dihydrochloride (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation[4].
Piribedil dihydrochloride (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 dihydrochloride (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11)[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability 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.
In Vivo

Piribedil dihydrochloride (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease[2].
Piribedil dihydrochloride (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets[3].
Piribedil dihydrochloride (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

371.26

Formula

C16H20Cl2N4O2

CAS No.
SMILES

C1(N2CCN(CC3=CC=C(OCO4)C4=C3)CC2)=NC=CC=N1.Cl.Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Piribedil dihydrochloride
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HY-12707A
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