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Product Name: PIRIBEDIL HYDROCHLORIDE
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78213-63-5

78213-63-5 structure

Name: PIRIBEDIL HYDROCHLORIDE
Chemical Name: 2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]pyrimidine,hydrochloride
CAS Number: 78213-63-5
Molecular Formula: C₁₆H₁₉ClN₄O₂
Molecular Weight: 334.80100
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2018-03-10 08:00:00
Modify Date: 2024-01-12 12:02:51
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].

Name	2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]pyrimidine,hydrochloride
Synonyms	Piribedil hydrochloride Piribedil Mono-hydrochloride Piribedil dihydrochloride

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].
Related Catalog	Research Areas >> Cancer Research Areas >> Endocrinology Signaling Pathways >> Epigenetics >> Histone Methyltransferase Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
Target	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]. 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]. 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.
References	[1]. Sweet RD, et al. Piribedil, a dopamine agonist, in Parkinson's disease. Clin Pharmacol Ther. 1974 Dec;16(6):1077-82. [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. [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. [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.

Boiling Point	469.4ºC at 760 mmHg
Molecular Formula	C₁₆H₁₉ClN₄O₂
Molecular Weight	334.80100
Flash Point	237.7ºC
Exact Mass	334.12000
PSA	50.72000
LogP	2.33240

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV9707200

CHEMICAL NAME :: Pyrimidine, 2-(4-piperonyl-1-piperazinyl)-, hydrochloride

CAS REGISTRY NUMBER :: 78213-63-5

LAST UPDATED :: 198602

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C16-H18-N4-O2.Cl-H

MOLECULAR WEIGHT :: 334.84

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 40,477,1985

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