Piribedil

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.