2. GPCR/G Protein Neuronal Signaling Epigenetics
  3. Adrenergic Receptor Dopamine Receptor Histone Methyltransferase
  4. 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.

For research use only. We do not sell to patients.

Piribedil dihydrochloride Chemical Structure

Piribedil dihydrochloride Chemical Structure

CAS No. : 1451048-94-4

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Piribedil dihydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Piribedil dihydrochloride

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α adrenergic receptor β adrenergic receptor

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

View All Histone Methyltransferase Isoform Specific Products:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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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[1]

α adrenergic receptor

 

D2 Receptor

 

D3 Receptor

 

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.

Piribedil dihydrochloride Related Antibodies

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Piribedil dihydrochloride Related Classifications

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Help & FAQs
  • 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.

Keywords:

Piribedil1451048-94-4Adrenergic ReceptorDopamine ReceptorHistone MethyltransferaseBeta ReceptorParkinson'sdyskinesiaslocomotor activityanti-leukemicMLL1THP-1MV4;11leukemiacancerInhibitorinhibitorinhibit

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