Home Neuronal Signaling Dopamine Receptor agonist - Adrenergic Receptor antagonist Piribedil For research use only.

Piribedil

Synonyms: Trivastal, Trivastan

Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.

Piribedil Chemical Structure

Piribedil Chemical Structure

CAS: 3605-01-4

Selleck's Piribedil has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.77%
99.77

Piribedil Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

Choose Selective Dopamine Receptor Inhibitors

Biological Activity

Description Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.
Targets
D3 receptor [3] adrenoceptor α2C [3]
(CHO)		 adrenoceptor α2A [3]
(CHO)		 D2 receptor [3]
(CHO)
7.2(pKi) 7.1(pKi) 6.9(pKi)
In vitro
In vitro Piribedil is a direct dopamine receptor agonist used for the treatment of Parkinson's disease and of other clinical disorders involving dysfunction of the dopaminergic system. Piribedil has 20 times higher affinity for dopamine D3 than for dopamine D2-like receptors, and very low affinity for the dopamine D1 receptor subtype in rat brain. Piribedil is a potent inhibitor at dopamine D3 receptors with affinity between 30 and 60 nM[1]. Although piribedil is not a potent agent, its affinity at hα2A- and hα2C-ARs was comparable to that at D2 receptors[3].
In Vivo
In vivo Piribedil (2.5-4.0 mg/kg s.c.) accelerates hippocampal NE synthesis, elevates dialysis levels of NE in hippocampus and frontal cortex, and blocks hypnotic-sedative properties of the α2-AR agonist xylazine[3]. Although a subchronic treatment with piribedil (0.1-2 mg/kg) is not effective, a dose of 0.3 mg/kg administered for 3 weeks significantly reverses the akinetic deficits produced by the striatal dopamine depletion and progressively improves attentional deficits. When coadministered with the dopamine prodrug L-DOPA (3 mg/kg), piribedil (0.3 mg/kg) promotes a rapid and full recovery of preoperative performance[2].
Animal Research Animal Models Wistar rats
Dosages 2.5-4.0 mg/kg
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01519856 Completed
Parkinson''s Disease
Desitin Arzneimittel GmbH
 June 2009 --
NCT00725478 Completed
Parkinson''s Disease
Desitin Arzneimittel GmbH
 January 2008 --

Chemical Information & Solubility

Molecular Weight 298.34 Formula

C16H18N4O2
CAS No. 3605-01-4 SDF Download Piribedil SDF
Smiles C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC=CC=N4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (197.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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