Piribedil

Catalog No.S3656 Batch:S365602

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Technical Data

Formula

C16H18N4O2

Molecular Weight 298.34 CAS No. 3605-01-4
Solubility (25°C)* In vitro DMSO 60 mg/mL (201.11 mM)
Ethanol 10 mg/mL (33.51 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Animal Study:[3]
  • Animal Models

    Wistar rats

  • Dosages

    2.5-4.0 mg/kg

  • Administration

    s.c.

Selleck's Piribedil has been cited by 2 publications

Social behavioral profiling by unsupervised deep learning reveals a stimulative effect of dopamine D3 agonists on zebrafish sociality [ Cell Rep Methods, 2023, 3(1):100381] PubMed: 36814839
Social behavioral profiling by unsupervised deep learning reveals a stimulative effect of dopamine D3 agonists on zebrafish sociality [ Cell Rep Methods, 2023, 3(1):100381] PubMed: 36814839

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.