ChemicalBook CAS DataBase List 1451048-94-4

1451048-94-4

Name	Piribedil dihydrochloride
CAS	1451048-94-4
Molecular Formula	C16H19ClN4O2
MDL Number	MFCD09971034
Molecular Weight	334.8
MOL File	1451048-94-4.mol

Chemical Properties

storage temp.	Store at RT
form	Powder
Water Solubility	Soluble to 25 mM in water

Hazard Information

Description

A direct dopamine agonist, in clinical use for treatment of dopaminergic system dysfunction. Recent work suggests that it is selective for the D3 subtype, for which it has 20 times higher affinity than for D2, and possesses no significant affinity for D1 receptors.

Uses

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].

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].

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.

IC 50

α adrenergic receptor; D₂ Receptor; D₃ Receptor

storage

Store at RT

References

[1] Sweet RD, et al. Piribedil, a dopamine agonist, in Parkinson's disease. Clin Pharmacol Ther. 1974 Dec;16(6):1077-82. DOI:10.1002/cpt19741661077
[2] Gerlach M, et al. The effect of piribedil on L-DOPA-induced dyskinesias in a rat model of Parkinson's disease: differential role of α(2) adrenergic mechanisms. J Neural Transm (Vienna). 2013 Jan;120(1):31-6. DOI:10.1007/s00702-012-0818-7
[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. DOI:10.1002/mds.10200
[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. DOI:10.1016/j.canlet.2018.05.034

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