| Identification | Back Directory | [Name]
2-(4-[1,3-BENZODIOXOL-5-YLMETHYL]-1-PIPERAZINYL)PYRIMIDINE MALEATE SALT | [CAS]
937719-94-3 | [Synonyms]
PIRIBEDIL, MALEATE
PIRIBEDIL MALEATE SALT
2-(4-[1,3-BENZODIOXOL-5-YLMETHYL]-1-PIPERAZINYL)PYRIMIDINE MALEATE
2-(4-[1,3-BENZODIOXOL-5-YLMETHYL]-1-PIPERAZINYL)PYRIMIDINE MALEATE SALT | [Molecular Formula]
C20H22N4O6 | [MDL Number]
MFCD02684412 | [MOL File]
937719-94-3.mol | [Molecular Weight]
414.41 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: >10mg/mL
H2O: >10mg/mL | [form ]
powder | [InChI]
1S/C16H18N4O2.C4H4O4/c1-4-17-16(18-5-1)20-8-6-19(7-9-20)11-13-2-3-14-15(10-13)22-12-21-14;5-3(6)1-2-4(7)8/h1-5,10H,6-9,11-12H2;1-2H,(H,5,6)(H,7,8)/b;2-1- | [InChIKey]
DKGOFBARSQSLOW-BTJKTKAUSA-N | [SMILES]
[H]\C(=C(/[H])C(O)=O)C(O)=O.C1Oc2ccc(CN3CCN(CC3)c4ncccn4)cc2O1 |
| Hazard Information | Back Directory | [Uses]
Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4]. | [Biological Activity]
A direct dopamine agonist; may be selective for the D3 subtype; no significant affinity for D1 receptors. | [References]
[1] Sweet RD, et al. Piribedil, a dopamine agonist, in Parkinson's disease. Clin Pharmacol Ther. 1974 Dec;16(6):1077-82. DOI:10.1002/cpt19741661077
[2] Gerlach M, et al. The effect of piribedil on L-DOPA-induced dyskinesias in a rat model of Parkinson's disease: differential role of α(2) adrenergic mechanisms. J Neural Transm (Vienna). 2013 Jan;120(1):31-6. DOI:10.1007/s00702-012-0818-7
[3] Smith LA, Tet al. Repeated administration of piribedil induces less dyskinesia than L-dopa in MPTP-treated common marmosets: a behavioural and biochemical investigation. Mov Disord. 2002 Sep;17(5):887-901. DOI:10.1002/mds.10200
[4] Xiong Zhang, et al. Piribedil disrupts the MLL1-WDR5 interaction and sensitizes MLL-rearranged acute myeloid leukemia (AML) to doxorubicin-induced apoptosis. Cancer Lett. 2018 Sep 1;431:150-160. DOI:10.1016/j.canlet.2018.05.034 |
|
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
SIGMA-RBI
|
| Tel: |
800 736 3690 (Orders) |
| Website: |
www.sigma-aldrich.com |
|