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].
Piribedil/双哌嘧啶 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Noise-induced loss of Inner Hair Cell synaptic ribbons model
Subcutaneous injection
10 mg/kg
3 days before and 3 days after, total 7 days
To assess if Piribedil could reduce noise-induced loss of Inner Hair Cell synaptic ribbons. Results showed that Piribedil alone significantly reduced ribbon loss in the 5.5 mm region but did not reach significance in the 6.5 mm region.
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