1. GPCR/G Protein Neuronal Signaling Epigenetics
  2. Dopamine Receptor Adrenergic Receptor Histone Methyltransferase
  3. Piribedil hydrochloride

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

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

Piribedil hydrochloride Chemical Structure

Piribedil hydrochloride Chemical Structure

CAS No. : 78213-63-5

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Description

Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase 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]

D2 Receptor

 

D3 Receptor

 

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].

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

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.
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].

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

334.80

Formula

C16H19ClN4O2

CAS No.
SMILES

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

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
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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 hydrochloride
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HY-12707C
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