Piribedil hydrochloride
Based on 1 publication(s) in Google Scholar
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.
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- CAS No.: 78213-63-5
- Formule: C16H19ClN4O2
- Masse moléculaire:334.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Piribedil hydrochloride
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Activité biologique
Description
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.
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Cell Line:MLL-r AML cells (THP-1 and MV4;11), non-MLL leukemia cell line (K562)
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Concentration:0, 20, 40, 80 and 160 μM
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Incubation Time:0-7 days
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Result:Inhibited the growth rate of the THP-1 and MV4;11 cells in a time-dependent manner.
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Cell Line:THP-1 and MV4;11 cells
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Concentration:0, 20, 40, 80 and 160 μM
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Incubation Time:4 days
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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 (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.
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Animal Model:Rat model of Parkinson’s disease[2]
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Dosage:5, 15, 40 mg/kg
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Administration:Intraperitoneal injection, administered 5 min before administration of L-DOPA.
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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.
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Animal Model:Adult common marmosets[3]
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Dosage:4-5 mg/kg
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Administration:Oral gavage, daily for 2 weeks
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Result:Increased vigilance and alertness and reversed the downregulation of preprotachykinin mRNA induced by MPTP in rostral and caudal striatum.
Chemical Information
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CAS No. 78213-63-5
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Masse moléculaire 334.80
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Formule C16H19ClN4O2
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SMILES
[H]Cl.C1(N2CCN(CC3=CC=C(OCO4)C4=C3)CC2)=NC=CC=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Chem
Terazosin Analogs Targeting Pgk1 as Neuroprotective Agents: Design, Synthesis, and Evaluation. [Abstract]2022 Jul 26:10:906974. PMID: 35958233
Pureté et documentation
Références
[1]. Sweet RD, et al. Piribedil, a dopamine agonist, in Parkinson's disease. Clin Pharmacol Ther. 1974 Dec;16(6):1077-82. [Content Brief]
[3]. Smith LA, Tet al. Repeated administration of piribedil induces less dyskinesia than L-dopa in MPTP-treated common marmosets: a behavioural and biochemical investigation. Mov Disord. 2002 Sep;17(5):887-901. [Content Brief]
[4]. Xiong Zhang, et al. Piribedil disrupts the MLL1-WDR5 interaction and sensitizes MLL-rearranged acute myeloid leukemia (AML) to doxorubicin-induced apoptosis. Cancer Lett. 2018 Sep 1;431:150-160. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Piribedil hydrochloride Related Classifications
HY-12707C Related Classifications
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