Piribedil

For research use only.

Catalog No.S3656 Synonyms: Trivastal, Trivastan

Piribedil Chemical Structure

CAS No. 3605-01-4

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

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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

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 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].

Protocol

Animal Research:[3]
- Collapse
  • Animal Models: Wistar rats
  • Dosages: 2.5-4.0 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 59 mg/mL (197.76 mM)
Water Insoluble
Ethanol '59 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.34
Formula

C16H18N4O2

CAS No. 3605-01-4
Storage powder
in solvent
Synonyms Trivastal, Trivastan
Smiles C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC=CC=N4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01519856 Completed Drug: piribedil (Clarium) Parkinson''s Disease Desitin Arzneimittel GmbH June 2009 --
NCT00725478 Completed Drug: Piribedil Parkinson''s Disease Desitin Arzneimittel GmbH January 2008 --

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Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID