2-(4-[1,3-BENZODIOXOL-5-YLMETHYL]-1-PIPERAZINYL)PYRIMIDINE MALEATE SALT

2-(4-[1,3-BENZODIOXOL-5-YLMETHYL]-1-PIPERAZINYL)PYRIMIDINE MALEATE SALT Property

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

Safety

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

WGK 3

Storage Class

11 - Combustible Solids

Hazard Classifications

Eye Irrit. 2
Skin Irrit. 2
STOT SE 3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

2-(4-[1,3-BENZODIOXOL-5-YLMETHYL]-1-PIPERAZINYL)PYRIMIDINE MALEATE SALT Chemical Properties,Usage,Production

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