Piribedil is a potent and orally active agonist for dopamine D2 and dopamine D3 receptors. Additionally, it acts as an antagonist for α2-adrenoceptors. Piribedil exhibits inhibition of MLL1 methyltransferase activity with an EC50 of 0.18 μM. Its potential applications include research related to Parkinson's disease, circulatory disorders, and cancers [1][2][3][4].
体内研究
Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) mitigates L-DOPA-induced dyskinesias in a rat model of Parkinson's disease [2].
Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) enhances locomotor activity and reverses motor deficits in adult common marmosets [3].
Piribedil (oral gavage, 150 mg/kg, daily for 21 days) suppresses MLL-r tumor growth and reduces the expression of MLL1 target genes in MV4;11 tumor xenografts [4].
体外研究
Piribedil, at concentrations ranging from 0 to 160 μM over a period of 7 days, exhibits specific inhibition of MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation [4].
Piribedil, administered at concentrations ranging from 0 to 160 μM for 4 days, specifically reduces H3K4 methylation in MLL-r cells (THP-1 and MV4;11) by disrupting the MLL1-WDR5 interaction [4].
Piribedil, administered at concentrations ranging from 0 to 160 μM for 4 days, triggers cell-cycle arrest, apoptosis, and differentiation in MLL-r cells (THP-1 and MV4;11) [4].
搜索
