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Piribedil Dopamine Receptor agonist

Name: Piribedil
Brand: Selleck Chemicals
SKU: S3656
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S3656

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

Chemical Structure

Molecular Weight: 298.34

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Quality Control

Batch: Purity: 99.77%

99.77

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Dopamine Receptor Products	MPTP Hydrochloride Trifluoperazine Trifluoperazine 2HCl Penfluridol SCH-23390 hydrochloride Domperidone SKF38393 HCl Sulpiride Azaperone C-DIM12

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (197.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	298.34	Formula	C₁₆H₁₈N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	3605-01-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Trivastal, Trivastan			Smiles	C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC=CC=N4

Mechanism of Action

Targets/IC₅₀/Ki	D3 receptor adrenoceptor α2C (CHO) 7.2(pKi) adrenoceptor α2A (CHO) 7.1(pKi) D2 receptor (CHO) 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. This compound 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. It is a potent inhibitor at dopamine D3 receptors with affinity between 30 and 60 nM. Although this chemical is not a potent agent, its affinity at hα2A- and hα2C-ARs was comparable to that at D2 receptors.
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. Although a subchronic treatment with this compound (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), this chemical (0.3 mg/kg) promotes a rapid and full recovery of preoperative performance.
References	[1] https://pubmed.ncbi.nlm.nih.gov/8905329/ [2] http://jpet.aspetjournals.org/content/jpet/319/2/914.full.pdf [3] https://pubmed.ncbi.nlm.nih.gov/11356907/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	--

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