Piribedil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Piribedil 是一种抗帕金森病化合物和哌嗪衍生物，可作为 D2 和 D3 受体激动剂。它还具有 α2-肾上腺素能拮抗剂特性

Piribedil is an antiparkinsonian agent andpiperazine derivative which acts as a D2 and D3 receptor agonist. It also has α2-adrenergic antagonist properties(In Vitro):Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation.Piribedil (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.Piribedil (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11).(In Vivo):Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease.Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets.Piribedil (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.

Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation.Piribedil (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.Piribedil (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11). Cell Proliferation Assay 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 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.

Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease.Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets.Piribedil (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. Animal Model:Rat model of Parkinson’s disease 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 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.

Piribedil | ET 495 | ET-495 | ET495 | EU 4200

Endocrinology/Hormones

Adrenergic Receptor

α2-adrenergic| D2| D3

Neurological Disease

——

3605-01-4

298.34

C16H18N4O2

>98% (HPLC)

Soluble in chloroform, DMSO, Ethanol, Water

C1(N2CCN(CC3=CC4=C(C=C3)OCO4)CC2)=NC=CC=N1

2-(4-Piperonyl-1-piperazinyl)pyrimidine

(-20℃)

With Ice Pack

≥ 2 years