Piribedil

Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers^[1][2][3][4]. IC50 & Target: D₂R, hα_1A-AR^[1]
EC50: 0.18 μM (MLL1 methyltransferase)^[4] In Vitro: Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation^[4].
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^[4].
Piribedil (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11)^[4].
In Vivo: Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease^[2].
Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets^[3].
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^[4].